159830-01-0Relevant academic research and scientific papers
An enantioselective approach to 4-substituted proline scaffolds: Synthesis of (s)-5-(tert-butoxy carbonyl)-5-azaspiro[2.4]heptane-6-carboxylic acid
Ariza, Xavier,Bartra, Martí,Berenguer, Ramon,Gómez, Roberto,Garcia, Jordi,López, Blanca,Torralvo, Hèctor
, (2021/06/14)
A catalytic and enantioselective preparation of the (S)-4-methyleneproline scaffold is described. The key reaction is a one-pot double allylic alkylation of an imine analogue of glycine in the presence of a chinchonidine-derived catalyst under phase transfer conditions. These 4-methylene substituted proline derivatives are versatile starting materials often used in medicinal chemistry. In particular, we have transformed tert-butyl (S)-4-methyleneprolinate (12) into the N-Boc-protected 5-azaspiro[2.4]heptane-6-carboxylic acid (1), a key element in the industrial synthesis of antiviral ledipasvir.
ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Paragraph 0760, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS
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Page/Page column 58, (2014/01/17)
The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement alternative inhibitors for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS
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Page/Page column 80, (2014/01/17)
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
A Short and Efficient Synthesis of (S)-4-Methylene Proline Benzyl Ester from (S)-Pyroglutamic Acid
Panday, Sharad Kumar,Griffart-Brunet, Dominique,Langlois, Nicole
, p. 6673 - 6676 (2007/10/02)
(S)-4-methylene proline benzyl ester 2 was synthesized from benzyl N-tert-butoxycarbonyl pyroglutamate through a Mannich and a Cope elimination reactions.
