Stereodivergent synthesis of both (2S)- and (2R)-1-monoricinolein derivatives by lipase-catalyzed hydrolysis or transesterification directed to new ferroelectric liquid crystals
摘要:
The preparation of both (2S)- and (2R)-1-monoricinolein derivatives has been developed to synthesize ferroelectric liquid crystals. Lipase-catalyzed hydrolysis of 2-protected-1,3-diricinoleins provided (2S)-1-monoricinolein derivatives with high diastereoselectivities, while transesterification of 2-protected glycerols with vinyl recinoleate gave (2R)-1-monoricinolein counterparts in good yields with high diastereoselectivities. (c) 2007 Elsevier Ltd. All rights reserved.
An Efficient Synthesis of 2-[(4-Amino∼1,2-dihyro-2-oxo-1- pyrimidinyl)methoxyi-l,3-propanediyl-di-L-valinate an Anti-cytomegalovirus Agent
摘要:
An efficient synthesis for large scale preparation of the titled compound, a prodrug for the anti-HCMV agent 1-[2-hydroxy-1-(hydroxymethyl)ethoxyl]cytosine, 9, has been developed. The product of each step is easily purified by either distillation or recrystallization and the final product is obtained in a high overall yield.
[EN] MACROCYCLIC COMPOUNDS AS STING AGONISTS AND METHODS AND USES THEREOF<br/>[FR] COMPOSÉS MACROCYCLIQUES UTILISÉS EN TANT QU'AGONISTES STING ET PROCÉDÉS ET UTILISATIONS DE CEUX-CI
申请人:LUPIN LTD
公开号:WO2021014365A1
公开(公告)日:2021-01-28
Disclosed are macrocyclic compounds having the general Formula (I) or (II) and their tautomeric forms, stereoisomers, pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof, and their combination with suitable medicament, corresponding processes for the synthesis and pharmaceutical compositions and uses of compounds disclosed herein.
[EN] MACROCYCLIC COMPOUNDS AS STING AGONISTS<br/>[FR] COMPOSÉS MACROCYCLIQUES UTILISÉS EN TANT QU'AGONISTES STING
申请人:LUPIN LTD
公开号:WO2020194160A1
公开(公告)日:2020-10-01
Disclosed are the macrocyclic compounds having the general Formula (I) and their tautomeric forms, stereoisomers, pharmaceutically acceptable salts, and their combination with suitable medicament, corresponding processes for the synthesis and pharmaceutical compositions and uses of compounds disclosed herein.
enantioselective acylative desymmetrization of glycerol was developed by using a chiral DMAP derivatives 1e having a 1,1ʹ-binaphthyl unit. The reactions required only 0.1 mol% of the catalyst and showed moderate to good enantioselectivity (up to 94:6 er). Control experiments revealed that the first acylation of a glycerol derivative proceeded selectively rather than the second acylation to give diacylate.