- On the origins of enantioselectivity in oxazaborolidine mediated carbonyl reductions
-
A series of tricyclic oxazaborolidine catalysts have been prepared from readily available (S)-indoline-2-carboxylic acid. In each case, an arene chromium(0) carbonyl group was introduced on one face of the catalyst. Results obtained in the borane mediated
- Jones, Graham B.,Heaton, Steven B.,Chapman, Brant J.,Guzel, Mustafa
-
-
Read Online
- Cis-fused ring-containing β-lactam the synthetic method of the compound of
-
The invention discloses a synthetic method of a beta-lactam compound with a cis condensed ring. Substituted or un-substituted pyrrole-2-formic acid, or substituted or un-substituted pyridine-2-formic acid or substituted or un-substituted indole-2-formic acid is used as a starting material, Pd(II) is adopted as a catalyst, and AgOAc or Ag2CO3 is used as an oxidant; a sp3C-H bond at a beta site of an amide substrate 2 (for example Scheme4) is activated through palladium catalysis; a key step of forming a C-N bond in a molecule to successfully construct a beta-lactam framework with the cis condensed ring is generated. According to the synthetic method disclosed by the invention, materials are simple and easily available, the price is cheap, the experiment operation is simple, the route is short and the yield is high; the synthetic method has very high atom economy, a little waste, environment friendliness, a wide scope of application of the substrate and good universality, and can be used for efficiently obtaining the beta-lactam compound with optical activity kept in a chiral manner.
- -
-
Page/Page column 2
(2016/12/01)
-
- ANTIMICROBIAL INDOLINE COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS
-
The present invention provides indoline heterocyclic compounds of the following formula I: or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods f
- -
-
Page/Page column 20-21
(2010/04/23)
-
- ANTIMICROBIAL HETEROCYCLIC COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS
-
The present invention provides heterocyclic compounds of the following formula (I) : or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
- -
-
Page/Page column 50
(2008/12/08)
-
- Tetrazolic acid functionalized dihydroindol: Rational design of a highly selective cyclopropanation organocatalyst
-
(Chemical Equation Presented) Herein we wish to report our development of an improved catalyst (S)-(-)-indoline-2-yl-1H-tetrazole (1) for the enantioselective organocatalyzed cyclopropanation of α,β-unsaturated aldehydes with sulfur ylides. The new organo
- Hartikka, Antti,Arvidsson, Per I.
-
p. 5874 - 5877
(2008/02/09)
-
- Both enantiomers of N-Boc-indoline-2-carboxylic esters
-
An immobilized form of Candida antarctica lipase (Chirazyme L-2) catalyzed enantioselective hydrolysis (E > 1000) of N-Boc-indoline-2-carboxylic acid methyl ester. The reaction proceeded efficiently at 60 °C, a temperature over the melting point of substrate, in the conversion of 49.9% to provide the hydrolyzed product, (S)-carboxylic acid with >99.9% ee and the unreacted (R)-ester with 99.6% ee. A newly developed expeditious route to the racemic substrate (a total of six steps, 60% yield), starting from aniline and ethyl α-methylacetoacetate, established the scalable chemoenzymatic synthesis of the desired compounds in both enantiomerically pure forms.
- Kurokawa, Masayuki,Sugai, Takeshi
-
p. 1021 - 1025
(2007/10/03)
-
- Tripeptidylpeptidase inhibitors
-
A compound of formula wherein the substituents are defined as in the specification and salts or hydrates thereof is disclosed as well as a method of treating disorders associated with the inactivation or excessive degradation of cholecystokinin.
- -
-
-
- Enantioselective addition of dialkylzinc to aldehydes catalyzed by (S)- 2-(N,N-disubstituted aminomethyl)indoline
-
Chirai di- or triamines, (S)-2-(N,N-disubstituted aminomethyl)indoline 1a-d, derived from (S)-indoline-2-carboxylic acid were efficient chiral catalysts for the enantioselective addition of dialkylzincs to aldehydes. The best results were obtained by empl
- Asami, Masatoshi,Watanabe, Hiroyasu,Honda, Kiyoshi,Inoue, Seiichi
-
p. 4165 - 4173
(2007/10/03)
-
- Process for the preparation of an indoline carboxylic acid
-
The invention relates to a novel process for the preparation of the optically pure 2S- or 2R-indolinecarboxylic acid of the formula STR1 and salts thereof. The process comprises forming the heterocyclic 5-membered ring in formula I from an open chain prec
- -
-
-
