ライフサイエンスコーパス: indoline

1 ne and therefore the rate of buildup of E(Q)(indoline).

2 followed by a very slow reappearance of E(Q)(indoline).

3 to the preparation of a 1,2,3-trisubstituted indoline.

4 e, E(A-A), is formed and the enzyme releases indoline.

5 the high local concentration of sequestered indoline.

6 ry-function studies of a series of bioactive indolines.

7 paration of 2,3-cis- and trans-disubstituted indolines.

8 xaldehyde with the appropriately substituted indolines.

9 antioselective synthesis of fused polycyclic indolines.

10 stereodiscriminations for most of the tested indolines.

11 dical-mediated regioselective bromination of indoline 12 serving as a key step.

12 group gave either tetrahydroquinolines 18 or indolines 14 in high overall yield and diastereoselectiv

13 We report that a series of novel indoline-2-carboxamides have been identified as inhibito

14 rahydroisoquinoline-3-carboxylate (Tic), and indoline-2-carboxylate.

15 unctionalized benzofuran and lactone bearing indoline-2-one scaffolds under same conditions.

16 ed dihydrothiopyrans has been developed from indoline-2-thiones.

17 described spiro[imidazo[1,5-c]thiazole-3,3'-indoline]-2',5,7(6H,7aH)-trione p53 modulators were prep

18 CFM-4 (1(2-chlorobenzyl)-5'-phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one), a lead compound

19 and 2,3-allenoate into enantioenriched spiro[indoline-3,2'-pyrrole] derivatives with a quaternary ste

20 as equivalents of alkynes to construct spiro[indoline-3,2'-pyrrole] structure.

21 '-(cyclohexane carbonyl)-1-methyl-2-oxospiro[indoline-3,2'-thiazolidine] (4n) emerged as the most pot

22 n this case, a 2'-isobutyl-substituted spiro[indoline-3,3'-pyrrolenine] results.

23 ous retro-Mannich fission to produce a spiro[indoline-3,3'-pyrrolenine] with relative configuration d

24 beta-phenyltropane, 6, and 1-methylspiro[1H-indoline-3,4'-piperidine], 7, were synthesized and teste

25 For most of the indoline-3-propionic acid derivatives, introduction of N

26 we prepared a large number of derivatives of indoline-3-propionic acids and esters.

27 rovides, among other products, indole 29 and indoline 30.

28 1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)-indoline-4-carbonitriles showed potent binding to the an

29 ome, which is formed through coupling at the indoline 5-position using redox chemistry, exhibits pH-g

30 Such a screen revealed sulfolane 1 and indoline-5-sulfonamides 2 and 3 as potent inhibitors of

31 s of enantiomerically enriched 2-substituted indolines, a substructure found extensively in both hete

32 or the construction of highly functionalized indolines, a substructure occurring in numerous biologic

33 red synthesis of a highly diverse polycyclic indoline alkaloid library, that selectively resensitizes

34 ycinyl imine to provide either enantiomer of indoline alpha-amino acids with high ee.

35 ew series of active and selective pyrimidone indoline amide PI3Kbeta inhibitors.

36 atile, amide-directed ortho-acetoxylation of indoline amides enabled our implementation of a unified

37 synthesis of a wide variety of chiral cyclic indoline aminals and indole aminals with aromatic and al

38 and efficient asymmetric synthesis of cyclic indoline aminals was developed with a high level of 1,3-

39 Dehydrogenation of the indoline aminals with potassium permanganate produced th

40 sformation (by making a benzologue) gave the indoline analogue, butabindide (33) as a reversible inhi

41 ange of synthetically important and advanced indoline analogues are selectively functionalized at the

42 oacrylate intermediate with the nucleophiles indoline and 2-aminophenol correlate with an upfield shi

43 labeling studies from the reactions of both indoline and acyclic arylamines with DCCPh showed that t

44 on/direct arylation cascade reaction between indoline and an arylated agent was efficaciously perform

45 o photochromic compounds incorporating fused indoline and benzooxazine fragments.

46 quickly through the quinonoid state to give indoline and the alpha-aminoacrylate Schiff base, E(A-A)

47 intermediate in rapid equilibrium with bound indoline and the E(A-A) intermediate before leaking out

48 ion limits the rate of accumulation of free indoline and therefore the rate of buildup of E(Q)(indol

49 is of chiral 2-bromo, chloro, and iodomethyl indolines and 2-iodomethyl pyrrolidines.

50 Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines w

51 iate conditions, can directly deliver varied indolines and hydroindolines through [4+2] cycloaddition

52 novel pyridyl- or isoquinolinyl-substituted indolines and indoles was designed via a ligand-based ap

53 and 4-pentenylsulfonamides to afford chiral indolines and pyrrolidines, respectively, was investigat

54 ce, which results in the synthesis of chiral indolines and pyrrolidines.

55 cycloaddition substrate for the synthesis of indolines and related heterocyclic systems.

56 idines, pyrrolidines, piperidines, azepanes, indolines and tetrahydroisoquinolines.

57 his method enables atom-economical access to indolines and tetrahydroquinolines in excellent yields,

58 The single-operation deracemization of 3H indolines and tetrahydroquinolines is described.

59 MVC-free E(A-A) gives very little E(Q)(indoline), and turnover is strongly impaired; the fracti

60 d proficiently constructs dihydrobenzofuran, indoline, and chroman skeletons of biological significan

61 of heterocyclic substrates including indole, indoline, and indazole afford the desired products in mo

62 construction of enantioenriched pyrrolidine, indoline, and piperidine rings using an organocatalyzed,

63 e used herein, the reactive indole analogue, indoline, and the l-Trp analogue, l-His.

64 action affords enantioenriched pyrrolidines, indolines, and gamma-amino-alpha,beta-unsaturated carbon

65 reas hydrogen bonding interactions probed by indoline are insensitive to solvent identity and instead

66 Indolines are important moieties present in various biol

67 2-Substituted indolines are resolved (s=2.6-19) using an atropisomeric

68 brium distribution strongly in favor of E(Q)(indoline) as a consequence of the high local concentrati

69 , hydroarylation reactions with formation of indolines, as well as intramolecular hydroaminations and

70 The Ru(II)-catalyzed C-H amidation of indoline at the C7-position en route for synthesizing th

71 ereocenter and represent an unusual class of indolines bearing structural resemblance to the hybrid n

72 nantioselective approach to the synthesis of indolines bearing two asymmetric centers, one of which i

73 + 2] cycloaddition to give the cyclopropa[c]indoline building block present in cycloclavine.

74 pallada(II)cycle, which is converted into an indoline by oxidative addition to the diaziridinone and

75 ed to synthesize azetidine, pyrrolidine, and indoline compounds via palladium-catalyzed intramolecula

76 unctionalized cyclopenta- or cyclohexa-fused indoline compounds, which are common structures of many

77 y enantioenriched 2,3-dihydrobenzofurans and indolines containing molecules from readily available su

78 he method provides access to benzofuran- and indoline-containing products.

79 Oxindoles and their indoline derivatives are common structural motifs found

80 rless dehydrogenation of tetrahydroquinoline/indoline derivatives in toluene (release of H2) at 130 d

81 uccessfully expanded for C7-acetoxylation of indoline derivatives using pyrimidine as a detachable di

82 A series of 1,6-disubstituted indoline derivatives were synthesized and evaluated as i

83 ve a rapid formation and dissipation of E(Q)(indoline) followed by a very slow reappearance of E(Q)(i

84 r is strongly impaired; the fraction of E(Q)(indoline) formed is <3.5% of that given by the Na(+)-bou

85 -geometry trends were observed in the chiral indoline-forming reactions.

86 th molecules fuses a benzooxazine ring to an indoline fragment and can be assembled efficiently in th

87 ovalent attachment of a cyanide anion to the indoline fragment is responsible for these transformatio

88 in the formation of the required pentacyclic indoline framework of the target alkaloid.

89 rmed E(Q)(indoline) occurs due to leakage of indoline from the closed system.

90 ine in the DIT reaction; however, leakage of indoline from the enzyme into solution still occurs.

91 The preparation of trans-2,3-disubstituted indolines from 1-azido-2-allylbenzene derivatives via a

92 d intermolecular 1,2-carboamination route to indolines from N-aryl ureas and 1,3-dienes that proceeds

93 simple synthesis of C(3)-N(1') heterodimeric indolines from the addition of indole nucleophiles to re

94 ly described series of 1-(3-pyridylcarbamoyl)indolines from which they evolved.

95 ver, when GP is bound to the alpha-site, the indoline generated by DIT cleavage in the first turnover

96 sphate (GP) binds and closes the alpha-site, indoline generated in the DIT reaction is trapped for a

97 olefination, arylation, and acetoxylation of indolines have been developed using nitrile-containing t

98 1,2-Disubstituted indolines have been prepared in fair to good yields by a

99 l diazoacetates results in the generation of indolines having quaternary substitution at C3 in high d

100 lindole has been prepared in four steps from indoline in 62% overall yield.

101 tic effect that greatly slows the leakage of indoline in the DIT reaction and enhances the trapping e

102 ificantly more effective than GP in trapping indoline in the DIT reaction; however, leakage of indoli

103 ables the synthesis of a range of polycyclic indolines in good yields and with high enantioselectivit

104 thesis of a variety of cis-2,3-disubstituted indolines in high yield and enantioeselectivity.

105 l/photoredox catalysis is used to synthesize indolines in one step from iodoacetanilides and alkenes.

106 talyzed interconversion of diastereoisomeric indolines in the presence of certain quaternary ammonium

107 Racemic indolines including a variety of structural motifs such

108 is formed at the beta-site, thereby trapping indoline inside.

109 3-indolyl)succinimide to give a key class of indoline intermediates that could be glycosylated stereo

110 tocol for the synthesis of 2,3-disubstituted indolines is described.

111 for the preparation of highly functionalized indolines is reported.

112 nds to the alpha-site and E(A-A) and/or E(Q)(indoline) is formed at the beta-site, thereby trapping i

113 synthesize DIT, the quinonoid species, E(Q)(indoline), is formed quickly, while in the reverse react

114 ith the analogous indolyl derivatives, spiro[indoline-isoquinolinoxazine] (3) and spiro[indoline-phen

115 In the forward reaction (indoline + L-Ser) to synthesize DIT, the quinonoid speci

116 Previously we discovered a tricyclic indoline, N-[2-(6-bromo-4-methylidene-2,3,4,4a,9,9a-hexa

117 of Z,E and E,E isomers; substitution of the indoline nitrogen with an N-benzyl group resulted in inc

118 oduce the C7 quaternary stereocenter and the indoline nucleus of the natural product's scaffold.

119 The decay of the transiently formed E(Q)(indoline) occurs due to leakage of indoline from the clo

120 ion (DIT cleavage), the accumulation of E(Q)(indoline) occurs very slowly.

121 A tricyclic indoline, Of1, was discovered to selectively potentiate

122 ion of the side chain nitrogen as part of an indoline or an indole ring.

123 ient syntheses of broadly useful substituted indolines or indoles.

124 The synthesis relies on a late stage indoline oxidation which does not racemize the product.

125 o[indoline-isoquinolinoxazine] (3) and spiro[indoline-phenanthrolinoxazine] (4) through XRD analysis

126 The success of the indoline pi-nucleophile that evolved through our studies

127 The indoline produced exits the enzyme via the tunnel out th

128 Very high regioselectivity for 3-substituted indoline products is obtained for both aliphatic and sty

129 all library of chiral, enantioenriched spiro(indoline-pyrimidine)-diones derivatives.

130 the chemically rich crystal structure of the indoline quinonoid intermediate in the pyridoxal-5'-phos

131 -A) reacts rapidly with indoline to give the indoline quinonoid species, E(Q)(indoline), which slowly

132 tanidin and a betalain analogue derived from indoline resulted as the most potent inactivators of lip

133 alkyl substitution at the C3 position of the indoline ring enhanced selectivity for the norepinephrin

134 ompounds bearing a 3,3-dimethyl group on the indoline ring, 9k, 9o,p, and 9s,t, exhibited potent inhi

135 In particular, spiropiperidine indoline-substituted diaryl ureas are described as poten

136 synthetic roquefortine C derivatives bearing indoline systems to their respective nitrones.

137 ted nitrogen-containing heterocycles such as indolines, tetrahydroquinolines, and tetrahydrobenzazepi

138 Simple benzo-fused nitrogen heterocycles (indolines, tetrahydroquinolines, and their homologues) u

139 ctive C-H functionalization of electron-rich indolines that are otherwise highly reactive toward elec

140 this pathway, we synthesized 120 polycyclic indolines that contain 26 distinct skeletons and a wide

141 s also support a mechanism for the escape of indoline through the alpha-site that is limited by ASL d

142 MVC-bound E(A-A) reacts rapidly with indoline to give the indoline quinonoid species, E(Q)(in

143 A novel method for the oxidation of indolines to indoles is described.

144 cting as a three-atom component to construct indoline units in a highly regio- and diastereoselective

145 mployed to synthesize the resorcinol and iso-indoline units, respectively, which were efficiently cou

146 -H activation/amination sequence for forming indolines using di-tert-butyldiaziridinone.

147 he enantioselective synthesis of tetracyclic indolines using silver(I)/chiral phosphoric acid catalys

148 ound to generate C(3) quaternary substituted indolines via a thionium ylide-initiated [3,3]-sigmatrop

149 approach for the synthesis of 3-substituted indolines via regio- and stereoselective SN2-type ring-o

150 The indoline was shown to be in equilibrium with the nine-me

151 The indolines were obtained from the corresponding indoles v

152 to give the indoline quinonoid species, E(Q)(indoline), which slowly converts to dihydroiso-l-tryptop

153 ) species to provide substituted indoles and indolines with high enantio-, regio-, and diastereoselec

154 m rhodium catalysis gives branched N-allylic indolines with high regio- and enantioselectivity.

155 provides densely functionalized cyclopenta[b]indolines with versatile vinyl and nitro-groups.