ライフサイエンスコーパス: amidation

1 lycosylated threonine, and * = COOH-terminal amidation).

2 y the acetyltransferase HolE to catalyze the amidation.

3 sequence, C-terminal lysine, and C-terminal amidation.

4 vestigated to elucidate the mechanism of the amidation.

5 inal glycine of small peptides for its later amidation.

6 thetic version only in missing of N-terminal amidation.

7 file was consistent with defective bile acid amidation.

8 ding blocks were assembled by thioacid amine amidation.

9 efficiently coupled using Grignard-mediated amidation.

10 orms Asn and Asn-tRNA(Asn) by tRNA-dependent amidation.

11 was found to be uniquely effective for this amidation.

12 e II with increasing receptor methylation or amidation.

13 g macrocyclic ynamides via an intramolecular amidation.

14 with both ends protected by acetylation and amidation.

15 of modification, with the dominant one being amidation.

16 ed with diaminobutane, resulting in carboxyl amidation.

17 a decrease was observed following C-terminal amidation.

18 evoid of a tryptophan residue and C-terminal amidation.

19 s been utilized as a directing group for the amidation.

20 as an essential coupling partner for the C-H amidation.

21 h beta-cyclodextrins (host moieties) through amidation.

22 cation, and alpha2,3-linked sialic acids via amidation.

23 lick chemistry or classic esterification and amidation.

24 in was synthesized by eight such reiterative amidations.

25 re higher in energy than the thiocarboxylate amidations.

26 a mechanism by which FXR regulates bile acid amidation, a critical component of the enterohepatic cir

27 enase (PAM) (EC 1.14.17.3) catalyzes peptide amidation, a crucial post-translational modification, th

28 lycan structure revealed a total loss of DAP amidation, a modification that was found in 80% of DAP r

29 Carboxyl-terminal amidation, a required post-translational modification fo

30 he rate-limiting enzyme for C-terminal alpha-amidation, a specific and necessary modification of secr

31 CARs demonstrated amidation activity for various acids and amines.

32 No peptide amidation activity was detected in PAM mutant embryos, a

33 The key steps of amidation, alcohol activation, and cyclization are all m

34 The synthesis featured a direct amidation and a Bischler-Napieralski reaction to form th

35 same diacyl derivatives of amide (i.e., both amidation and acylation) in high yield was also demonstr

36 directly inhibits Src kinase by simultaneous amidation and ADP ribosylation of the conserved kinase-d

37 mild, regioselective, iridium-catalyzed C-H amidation and borylation of anthraquinones to the o-sulf

38 oquinone fragments proved unsuccessful, both amidation and C-N bond formation tactics with the more e

39 icipated, highly conserved link between PAM, amidation and ciliary assembly.

40 nce in products formed from copper-catalyzed amidation and copper-catalyzed ODC, reactions of an alky

41 ere coupled together at a late stage through amidation and cross-metathesis in a convergent manner.

42 employed as suitable acyl transfer agents in amidation and esterification in organic synthesis.

43 This allows the sequential amidation and generation of asymmetric squaramides with

44 azole is also generated in good yields using amidation and intramolecular aromatic nucleophilic subst

45 istinct multistep continuous-flow processes (amidation and Mg-I exchange/nucleophilic addition) to de

46 e targeted compounds through frequently used amidation and oxygenation processes in the academia and

47 r used as an electrophile enabled sequential amidation and provided asymmetric squaramides with high

48 ve gamma-C(sp(3))-H arylation/intramolecular amidation and the construction of both C-C and C-N bonds

49 ooxygenase (PAM), the enzyme responsible for amidation and therefore activation of all amidated neuro

50 tization by dimethylamidation and subsequent amidation and transferred this onto formalin-fixed paraf

51 en used for further transformations, such as amidations and Fukuyama coupling reactions.

52 Amidations and multicomponent reactions expanded the arm

53 minal residues after proteolysis, C-terminal amidation, and a unique post-translational modification,

54 ed as a coupling reagent for esterification, amidation, and dehydration of carboxylic acids (aliphati

55 conjugation techniques, reductive amination, amidation, and Huisgen cycloaddition, were employed for

56 genase (PAM) are essential for peptide alpha-amidation, and the cytosolic domain (CD) is essential fo

57 mide starting compounds are detailed, as are amidation approaches installing the alpha-ketoamide resi

58 Both type I and type II amidations are utilized in this effort, allowing access

59 lycan structures conserved in Acetobacteria: amidation at the alpha-(l)-carboxyl of meso-diaminopimel

60 y neuropeptides and peptide hormones require amidation at the carboxyl terminus for activity.

61 Direct ortho amidation at the phenyl ring of 2-phenylimidazo heterocy

62 culate forms and demonstrated that even with amidation-based shell cross-linking the core domain rema

63 bon nanotubes (MWCNTs) via diimide-activated amidation between the carboxyl groups on the CNT surface

64 asymmetric Michael-Michael-Mannich-reduction-amidation-Bischler-Napieralski-reduction reactions with

65 precursors frequently includes COOH-terminal amidation by the bifunctional enzyme peptidylglycine alp

66 equence (azide-alkyne cycloaddition/Goldberg amidation/Camps cyclization/(CH arylation)) for the rapi

67 ents, genetic defects that disrupt bile acid amidation cause fat-soluble vitamin deficiency and growt

68 ia coli type 1 pilus adhesin FimH(A) through amidation chemistry to enable bladder epithelial cell bi

69 The fifth ring was completed by a "one-pot" amidation-cyclization process promoted by palladium acet

70 three steps utilizing a palladium-catalyzed amidation/cyclization strategy.

71 Bile acid amidation defects were predicted to present with fat/fat

72 inborn errors of bile acid metabolism due to amidation defects.

73 trahydoisoquinoline ring, which upon further amidation, deprotection, and sulfation gave the targeted

74 a novel method to quantify SCFAs by coupling amidation derivatization of SCFAs with paper-loaded dire

75 Amidation derivatizes all sialic acids regardless of lin

76 from four families with defective bile acid amidation due to a genetically confirmed deficiency in b

77 e carboxyl group of this arginine residue by amidation, eliminated the binding and internalizing acti

78 Elaboration of the lactam cores via amidation enabled synthesis of novel ACC inhibitors and

79 lly, an aldehyde group was introduced by C-H amidation, enabling oxime ligation for the installation

80 zyme pair and highlights the first oxidation-amidation enzymatic cascade reaction leading to the sele

81 lude two well-established LDCV proteins, the amidation enzyme PHM and the ascorbate-regenerating elec

82 ost-synthetic modification reactions, namely amidation, esterification, and thioesterification, were

83 red via 1,3-dipolar cycloaddition (CuAAC) or amidation/esteryfication reactions.

84 etic transformations such as esterification, amidation, etc., highly efficient and modular simultaneo

85 Different amidation events on chromogranin A, and on peptides proc

86 nitial N-heterocyclic carbene mediated redox amidation exploying these two types of building blocks r

87 Many neuropeptides require amidation for full activation by peptidylglycine alpha-a

88 intermolecular branch-selective allylic C-H amidation has been accomplished via Ir(III) catalysis.

89 Palladium-catalyzed oxidative amidation has been used to synthesize hydroxamic acid-co

90 he stabilization of the helical structure by amidation has previously been shown to play a key role i

91 tion, Kornblum oxidation, and intramolecular amidation in a single reactor.

92 nowledge, the occurrence of C-terminal alpha-amidation in mAbs has not been reported previously.

93 We report here that amidation in mild acidic conditions can be used to neutr

94 quential iodination, Kornblum oxidation, and amidation in one pot.

95 Esterification or amidation in solution effectively protects sialic acids,

96 netic and biochemical basis for the terminal amidation in thiotetroamide C biosynthesis, which involv

97 eloping Drosophila melanogaster larvae, FMRF amidation in thoracic ventral (Tv) neurons is strikingly

98 C-terminal amidation in vivo was achieved by extending the sCT by a

99 es catalyzed transesterifications as well as amidations in a manner similar to those of previously re

100 When tested against Escherichia coli, amidation increased toxicity 10-fold (MIC = 31.25 muM) w

101 echanistic and DFT studies indicate that C-H amidation involves H-atom abstraction from R-H substrate

102 s for the neuropeptide amidating enzyme PHM; amidation is a highly specific and widespread modificati

103 alpha-Amidation is essential for the function of many peptides

104 t in human, mouse, and insect cells, peptide amidation is exquisitely sensitive to hypoxia.

105 esults indicate that, in Drosophila, peptide amidation is required for neuropeptide regulation of beh

106 Whether the most important effect of peptide amidation is the change in charge or an enhancement of h

107 The preferred site for amidation is the free carboxyl group of the meso-diamino

108 hage-display platform to select for specific amidation, leading to an order of magnitude acceleration

109 although the pathway must involve chelation, amidation, macrocyclic ring reduction, lactamization and

110 could be expected if any alternative peptide amidation mechanism exists in the mouse.

111 An efficient amidation method between readily available 1,1-dicyanoal

112 tivates the development of catalytic, direct amidation methods employing free carboxylic acids and am

113 compared, the latter undergoing Rh-catalyzed amidation more rapidly.

114 Reduced AP-1 function made 18-kDa fragment amidation more sensitive to inhibition by bathocuproine

115 to build the dapdiamide antibiotic scaffold, amidation must occur on the fumaroyl-DAP scaffold, after

116 oselective NHC-catalyzed dimerization and an amidation/N-acyliminium ion cyclization sequence to furn

117 s required for cellular respiration, peptide amidation, neurotransmitter biosynthesis, pigment format

118 -nitrogen bond-forming reactions (amination, amidation, nitration and nitrosation) that involve the u

119 c activity for the intramolecular C(sp(3))-H amidation of 1,4,2-dioxazol-5-ones to provide chiral gam

120 A Rh-catalyzed ortho-amidation of 2-aryloxazolines offers an efficient and di

121 The Ru(II)-catalyzed amidation of 2-arylpyridines with aryl isocyanates via C

122 could be applied toward the selective ortho amidation of 2-heteroarylimidazo[1,2-a]pyridine framewor

123 ates were synthesized using copper-catalyzed amidation of 3-amino-N-Boc-4-chloropyridine.

124 o[5.4.0]undec-7-ene-catalyzed intramolecular amidation of 7-arylindoles with diazomalonates is descri

125 e the Cu(II)-catalyzed C-H methoxylation and amidation of a macrocylic arene substrate with O(2) as t

126 curred in OSN, is attributable to C-terminal amidation of a natural peptide derived from osteocalcin.

127 ing to such a compound include the oxidative amidation of a phenol, a Cu(II)-catalyzed cyclocondensat

128 l, is as an effective reagent for the direct amidation of a variety of carboxylic acids with a broad

129 e method is efficient and allows for the C-H amidation of a wide range of functionalized thioamides w

130 Amidation of a wide variety of carboxylate salts with ei

131 ent-free cross-coupling method for oxidative amidation of aldehydes and alcohols via a metal-free rad

132 A practical method for the amidation of aldehydes with economic ammonium chloride o

133 The intramolecular dehydrogenative amidation of aliphatic amides, directed by a bidentate l

134 Notably, chemoselective amidation of aliphatic amines takes place in the presenc

135 es)Pd(TFA)2(H2O)-catalyzed aerobic oxidative amidation of alkene.

136 lective Pd-catalyzed "Wacker-type" oxidative amidation of alkenes.

137 onds is a key step in Pd-catalyzed oxidative amidation of alkenes.

138 nvolves the visible-light-promoted oxidative amidation of amines with pyrazole to synthesize N-acyl p

139 cation of the phytosphingosine side chain by amidation of an advanced methyl ester precursor.

140 ther demonstrates a challenging Cu-catalyzed amidation of an ortho-substituted aryl chloride.

141 roamide C involving the tandem oxidation and amidation of an unreactive ethyl group.

142 A Rh(III)-catalyzed protocol for the amidation of anilide and enamide C-H bonds with isocyana

143 We present results on the amidation of aryl halides and sulfonates utilizing a mon

144 ensive catalyst system was developed for the amidation of aryl halides by using 0.2-10 mol % of CuI,

145 d minimal impact on DNA polymerase function, amidation of Asp-358, Glu-401, and Asp-426 eliminated Mg

146 -tRNA formation in most prokaryotes requires amidation of Asp-tRNA or Glu-tRNA by amidotransferases t

147 The amidation of Asp69 and Glu119 caused a 7.6- and 88-fold

148 amidation of N-pyrimidylindolines and ortho-amidation of benzamides.

149 , this is the first report for the oxidative amidation of benzylamines and decyanation of benzyl cyan

150 genase (PAM) catalyzes the carboxyl-terminal amidation of bioactive peptides through a two-step react

151 nctional enzyme, catalyzes the COOH-terminal amidation of bioactive peptides.

152 A novel Ni-catalyzed reductive amidation of C(sp(2))-O and C(sp(3))-O electrophiles wit

153 um catalyzes the glutamine and ATP-dependent amidation of carboxylates b, d, e, and g within adenosyl

154 Direct amidation of carboxylic acids by reaction with amines in

155 m glutamicum (LtsACg) in the modification by amidation of cell wall peptidoglycan diaminopimelic acid

156 Finally, PyfP and PyfT are shown to catalyze amidation of CHPR to pyrazofurin 5'-phosphate thereby es

157 In this work, the first C(sp(2) )-H amidation of dehydroalanine (Dha) residues was applied t

158 Kinetic and computational studies on the amidation of esters with mixtures of formamide and sodiu

159 min(-1)); and (iii) FdmV also catalyzes the amidation of FDM M-3, a structural analog of FDM C, to a

160 tion and successive arylation/intramolecular amidation of gamma-C(sp(3))-H bonds.

161 that most Bacteria form Gln-tRNA(GLN) by the amidation of Glu-tRNA(GLN), only a few members of the ga

162 glucosamine is produced enzymatically by the amidation of glucose 6-phosphate and can then be further

163 ha-amidating enzyme catalyzes the C-terminal amidation of glycine-extended peptides.

164 zes the first step leading to the C-terminal amidation of glycine-extended peptides.

165 A cobalt-catalyzed C2-selective amidation of indoles using acyl azides has been accompli

166 The Ru(II)-catalyzed C-H amidation of indoline at the C7-position en route for sy

167 ed into known biosynthetic pathways, for the amidation of known acceptor molecules (e.g. CTP synthesi

168 ry over tertiary C-H bond selectivity in the amidation of linear and cyclic hydrocarbons with aroyl a

169 tial enzyme that catalyzes the COOH-terminal amidation of many neuroendocrine peptides.

170 For the amidation of N-acetylglycine, N-(tert-butoxycarbonyl)gly

171 The amidation of N-protected amino acids with both primary a

172 catalytic method is also applicable for C-7 amidation of N-pyrimidylindolines and ortho-amidation of

173 In this route, the amidation of NaMN to nicotinamide mononucleotide (NMN) o

174 copper-containing enzyme that catalyzes the amidation of neuropeptides hormones, the first step of w

175 minotransferase domain to supply ammonia for amidation of nicotinic acid adenine dinucleotide (NaAD(+

176 -quinolones that utilizes a copper-catalyzed amidation of o-halophenones followed by a base-promoted

177 d raise the possibility that region-specific amidation of PAM substrates contributes significantly to

178 -extended propeptides, the first step in the amidation of peptide hormones by the bifunctional enzyme

179 ooxygenase (PAM) catalyzes the COOH-terminal amidation of peptide hormones.

180 wo-step reaction resulting in the C-terminal amidation of peptides, a process important for their sta

181 Amidation of Phe-Met-Arg-Phe-amides, a group of cardiomo

182 nts of the catalyst allow for chemoselective amidation of primary amines in the presence of secondary

183 was explored as an amidating reagent for C8-amidation of quinoline N-oxide for the first time.

184 A cobalt(III)-catalyzed C-8 selective C-H amidation of quinoline N-oxide using dioxazolone as an a

185 I)-catalyzed protocol for C8-bromination and amidation of quinoline N-oxide was developed.

186 s been developed based on chelation-assisted amidation of readily available aryl boronic acids at roo

187 Novozym 435 mediated amidation of sophorolipid ethyl ester in dry THF with ph

188 o-beta-ketoesters is developed via oxidative amidation of sp, sp(2), and sp(3) C-H bonds.

189 The Ir(III)-catalyzed direct allylic C-H amidation of substituted internal alkenes with substitut

190 and binds to the same catalytic site for the amidation of the a-carboxylate.

191 ng muramyl tripeptides, were not affected by amidation of the alpha-carboxylic acid of iso-glutamic a

192 modification at W61, cyanylation at C56, and amidation of the C terminus at G63.

193 terminus and protonation, deprotonation, or amidation of the C terminus.

194 monstrate that CbiA catalyzes the sequential amidation of the c- and a-carboxylate groups of cobyrini

195 alytic mechanism in which CbiA catalyzes the amidation of the c-carboxylate, and then the intermediat

196 of the many bioactive peptides that require amidation of the carboxy terminus for full potency.

197 initial enzymatic adenylation of substrates, amidation of the carboxylic acid proceeds by direct reac

198 Furthermore, amidation of the d-Glu residue did not alter NOD2 activa

199 tion and successive arylation/intramolecular amidation of the gamma-C(sp(3))-H bonds.

200 inyl-tRNA(Asn) were likely formed in LUCA by amidation of the mischarged species, glutamyl-tRNA(Gln)

201 acteria by a pretranslational tRNA-dependent amidation of the mischarged tRNA species, Glu-tRNA(Gln)

202 -tRNA and asparaginyl-tRNA by tRNA-dependent amidation of the mischarged tRNA species, glutamyl-tRNA(

203 Amidation of the oxime ester (23b) with histamine, follo

204 s leucine methyl ester and performs a direct amidation of the polyketide, a reaction typically cataly

205 ctive desymmetrization via remote C(sp(2))-H amidation of the prochiral 2,2-disubstituted cyclopenten

206 iverdin reductases are less accommodating to amidation of the propionic acid side chains of biliverdi

207 n of O-methyl bromotyrosine methyl ester and amidation of the resulting oxime ester (14) with histami

208 n of a chiral oxime ether and chemoselective amidation of the resulting unprotected pipecolic acid.

209 gainst PC2 nearly 3-fold, whereas C-terminal amidation of the same peptide increased the potency by a

210 Many bioactive peptides require amidation of their carboxy terminus to exhibit full biol

211 NA(Asn) or Glu-tRNA(Gln), and the subsequent amidation of these amino acids while they are bound to t

212 -amidating monooxygenase (PAM) catalyzes the amidation of these diverse physiological regulators.

213 nt-free, and selective Cp*Co(III) -catalyzed amidation of thioamides with robust dioxazolone amidatin

214 A catalytic protocol for the base-mediated amidation of unactivated esters with amino alcohol deriv

215 are of unknown function, likely involved in amidation of unknown acceptors.

216 e proposed intermediates in copper-catalyzed amidations of aryl halides, have been synthesized and ch

217 used to gain an insight into the effects of amidation on antimicrobial selectivity.

218 acteria such as Escherichia coli by a single amidation on the peptide side chain.

219 ny that are not compatible with Pd-catalyzed amidation or amination methodology.

220 eutralization of inhibitor charged groups by amidation or esterification.

221 Carboxy-terminal amidation or substitution of tryptophan for tyrosine enh

222 immobilizing short recognition sequences by amidation or thiol-maleimide reactions.

223 1_2.1 enzyme may activate SLs (e.g. GR24) by amidation, or more likely could embody a new pathway for

224 r functionalization via reductive amination, amidation, or other chemistry.

225 t is proposed that this residue enforces the amidation order in the wild type enzyme via charge-charg

226 However, the strict amidation order observed with the wild type CbiP is part

227 utated to address the molecular basis of the amidation order; however, no changes in the order of ami

228 that the advantages conferred by C-terminal amidation outweigh increased amyloidogenicity.

229 post-translationally modified peptides (e.g. amidation, oxidation, lipidation, glycosylation or d-ami

230 arbon position through the diamide and alpha-amidation pathways.

231 dal anti-inflammatory drug, indomethacin, by amidation presents a promising strategy for designing no

232 A useful modification of the Weinreb amidation procedure was applied to the opening of the in

233 ocatalyst in a Cp*Rh(III)-catalyzed C-H bond amidation proceeding by an intramolecular amide transfer

234 The stereoselective amidation proceeds without additional acyl transfer agen

235 nd the target amide using an isodesmic trans-amidation process and is calibrated relative to 1-aza-2-

236 ial role of molecular sieves in this complex amidation process.

237 ogrammed cell death, we demonstrated that an amidation reaction between thio acids and sulfonyl azide

238 This novel amidation reaction involves a catalytic protocol using c

239 In vertebrates, the two-step peptide alpha-amidation reaction is catalyzed sequentially by two enzy

240 The selenocarboxylate/azide amidation reaction is clean and chemoselective.

241 This amidation reaction is operationally straightforward and

242 A simple, one-step amidation reaction is used to produce a range of 12-arm

243 ey step involves a novel palladium-catalyzed amidation reaction of 4-chloro-1-methylindazole 8 with t

244 d in good to very good isolated yields by an amidation reaction of different 2-haloanilines with 2-ca

245 umented is an intramolecular copper-mediated amidation reaction to close the 19-membered macrolactams

246 documented; however, it is very rare for an amidation reaction to occur without activation.

247 duce diphthine and allows the Dph6-catalyzed amidation reaction to occur.

248 The amidation reaction was also employed for the generation

249 hiometric versions of the Ir and Rh-mediated amidation reaction were compared systematically to each

250 gating a subsequent lanthanum(III)-catalyzed amidation reaction, a new multicomponent reaction was de

251 traightforward click coupling followed by an amidation reaction, and the siRNA delivery protocol requ

252 mide synthetase catalyzing the ATP-dependent amidation reaction.

253 ation of a charge-carried reagent through an amidation reaction.

254 polycaprolactone (PCL) bead surfaces through amidation reaction.

255 etween rMETase molecules during the carboxyl amidation reaction.

256 t perform unprecedented enantioselective C-H amidation reactions and control the site selectivity to

257 a has recently been shown to catalyze direct amidation reactions at room temperature in the presence

258 ligand, and base as the catalyst system, the amidation reactions proceed in good yields for a range o

259 rming reaction differs from that of standard amidation reactions, highlighting the ability to control

260 s has been carried out by esterification and amidation reactions.

261 The method is also useful for direct amidation reactions.

262 odification of NCNDs, such as alkylation and amidation reactions.

263 ontaining dyes via zero-length cross-linking amidation reactions.

264 tion of both intra- and intermolecular vinyl amidation reactions.

265 ns elucidate the origins of the superior C-H amidation reactivity displayed by the non-C(2)-symmetric

266 tide LLRVKR against furin 8-fold, C-terminal amidation reduced the potency < 2-fold.

267 a-amidating monooxygenase (PAM), and lack of amidation renders most of these peptides biologically in

268 Amidation requires conversion of a glycine-extended pept

269 ariation in the degree of esterification and amidation, respectively, had negligible effects.

270 having similar degrees of esterification and amidation, respectively.

271 , in the reaction of aryl-alkyl alkenes, the amidation selectively takes place at the alkyl-substitut

272 equired to achieve primary and secondary C-H amidation selectivity in the absence of directing groups

273 A condensation/amidation sequence converts alpha-boryl aldehydes into s

274 t desilylation/dihydropyranone fragmentation/amidation sequence.

275 acid N-terminal propeptide, and a C-terminal amidation signal.

276 of the resulting ester-amide after the first amidation step of the diester.

277 ctive peptides ends with an obligatory alpha-amidation step that is catalyzed only by peptidylglycine

278 e diphthamide synthetase catalyzing the last amidation step using ammonium and ATP.

279 46W or human WDR85) are involved in the last amidation step, with Dph6 being the actual diphthamide s

280 glycan using the solid-phase esterification/amidation strategy.

281 tivity of Co(III) -catalyzed C(sp(2) )-H Dha amidation suggests that this approach could be generaliz

282 orophenylselenide ring opening, and finally, amidation to afford the ring-D synthon 45 having the pro

283 late-stage intramolecular copper(I)-mediated amidation to complete the assembly of the tetracyclic fr

284 by a nickel-specific chelatase, followed by amidation to form Ni-sirohydrochlorin a,c-diamide.

285 Amidation to generate the physiologically relevant form

286 -alkylation and arylation, deprotection, and amidation to install broad molecular diversity in short

287 properties of proteins, as demonstrated with amidation to modify protein isoelectric point and throug

288 nic acid dinucleotide (NaAD) followed by its amidation to NAD, constitute promising drug targets for

289 tionally simple method for effecting allylic amidation using an environmentally benign oxidant and a

290 The (V/K)app for N-acylglycine amidation varies approximately 1000-fold, with the (V/K)

291 owed by concomitant C(sp(3))-H oxidation and amidation via oxidative C-C bond cleavage under an O(2)

292 monstrated that sequential deoxofluorination/amidation was possible.

293 tion, which is the key step of catalytic C-H amidation, was investigated in an integrated experimenta

294 Specifically, by polymer-analogous amidation we conjugated imidazole groups to the epsilon-

295 e enamide side chain and tandem deallylation/amidation were employed in synthetic routes to these der

296 n order; however, no changes in the order of amidation were obtained.

297 HATU-mediated amidation with glycine-OMe resulted in dipeptide (6).

298 thraquinone carbonyl moieties direct the C-H amidation with high selectivity to afford the ortho-subs

299 rmediate, followed by a subsequent oxidative amidation with readily available dioxazolones as nitreno

300 Little N-acyl amidation (with glycine or taurine) occurred.