专利号:US-7288661-B2 优先权日:2003-12-10 标 题 :Process for the synthesis of (2S,3aS,7aS)-1-[(S)-alanyl]-octahydro-1H-indole-2-carboxylic acid compounds and application in the synthesis of perindopril 发明人:DUBUFFET THIERRY; LECOUVE JEAN-PIERRE 权利人:SERVIER LAB 摘要:Process for the synthesis of compounds of formula (I): n nwherein R represents a hydrogen atom or a protecting group for the amino function.n n Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
专利号:US-2009131688-A1 优先权日:2007-11-21 标 题 :Method for the synthesis of 4-benzofuran-carboxylic acid 发明人:BURGOS ALAIN; MARUANI MARTINE; PERRIN FLORENCE; FREIN STEPHANE 权利人:ZACH SYSTEM 摘要:The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. n This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: n n n n n n n n n n wherein R independently represents hydrogen or a linear or branched C 1 - 15 alkyl group. n With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.
专利号:EP-2666771-A1 优先权日:2012-05-24 标题 :Synthesis of Aminocyclopentanetriol Derivatives 发明人:STERK DAMJAN; CASAR ZDENKO 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor. nThe present invention provides in particular a process for the preparation of a compound of formula Vn ncomprising: na) providing a compound of formula IVn n, and nb) reducing the compound of formula IV with activated zinc in the presence of copper to give the compound of formula V.
专利号:US-9278972-B2 优先权日:2011-12-23 标题 :Synthesis of triazolopyrimidine compounds 发明人:MARAS NENAD; GAZIC SMILOVIC IVANA; STERK DAMJAN 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:US-7173059-B2 优先权日:2003-05-08 标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same 发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN 权利人:AGOURON PHARMA 摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
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