专利号:US-4026911-A 优先权日:1976-02-23 标 题:Process for the preparation of ketoalkynoic acids and use of the process in an improved synthesis of 2-(substituted)-cyclo-pentane-1,3,4-triones 发明人:REVERMAN LAWRENCE FRANCIS 权利人:MILES LAB 摘要:Reaction of a 2-methyl-2-(alkenyl)-1,3-dioxolane with an α,ω-dihalogenoalkane to obtain a 2-methyl-2-(ω-chloroalkynyl)-dioxolane, conversion of the latter to a corresponding nitrile, and hydrolysis of the nitrile to form a ketoalkynoic acid is a novel process for preparing the acid. n Use of the process in the synthesis of 2-(substituted)-cyclopentane-1,3,4-triones improves that synthesis.
专利号:US-7935837-B2 优先权日:2008-04-30 标 题:Process for synthesis of androstane 17-β carbothioic acid and relative compounds thereof 发明人:HSU NAI-HSUAN; PANG CHU-YI; WU CHIEN-JEN; HUANG CHI-JEN; HSU CHIA-JUNG; LEE PEIMIN 权利人:CORUM INC 摘要:A process for synthesis of androstane 17-β carbothioic acid is provided. The process includes mixing an androstane 17-β carboxylic acid and a coupling reagent, and adding an alkanethioic acid to form an androstane 17-β carbothioic acid, wherein the androstane 17-β carbothioic acid has the formula (I): n n n n n n n n n n n n wherein R 1 represents hydrogen or haloalkyl groups, R 2 represents C 1-8 linear alkyl groups, C 1-8 branched alkyl groups, C 1-6 unsaturated acyclic groups or aromatic groups, R 3 represents hydrogen or hydroxyl, R 4 represents hydrogen, bromine, chlorine or fluorine and R 5 represents hydrogen, bromine, chlorine or fluorine. The process is a one-pot reaction.
专利号:US-2025066296-A1 优先权日:2021-12-14 标题 :Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; PHADKE AVINASH; RAI U SANKAPPA; CHANDRAN PRABU 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
专利号:US-7189864-B2 优先权日:1990-11-19 标 题:Method of preparing intermediates useful in synthesis of retroviral protease inhibitors 发明人:NG JOHN S; PRZYBYLA CLAIRE A; MUELLER RICHARD A; VAZQUEZ MICHAEL L; GETMAN DANIEL P 权利人:SEARLE & CO 摘要:A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
专利号:US-8927739-B2 优先权日:2011-05-18 标 题 :Processes for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives 发明人:QIU YAO-LING; PENG XIAOWEN; KIM IN JONG; CAO HUI; TANG DATONG; OR YAT SUN; WANG GUOQIANG; XU GUOYOU 权利人:ENANTA PHARM INC 摘要:The present invention relates generally to an improved process for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of hepatits C virus NS5A inhibitors. In particular, the present invention relates to processes and intermediates for the preparation of compounds of formulae (Ia), (Ib) and (Ic):
专利号:US-6022996-A 优先权日:1990-11-19 标 题 :Method for making intermediates useful in synthesis of retroviral protease inhibitors 发明人:NG JOHN S; PRZYBYLA CLAIRE A; MUELLER RICHARD A; VAZQUEZ MICHAEL L; GETMAN DANIEL P 权利人:SEARLE & CO 摘要:A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
[参考文献]: Thomas J Preston, Et Al. Formation And Relaxation Dynamics Of Iso-Ch2Cl-I In Cryogenic Matrices. J Chem Phys. 2011 Sep 21;135(11):114503.
合成参考文献
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