CAS: 32634-68-7; Di-P-Toluoyl-D-Tartaric Acid

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CAS号339546-21-3 (R)-2-cycloprop... | CAS号32634-66-5 L-二对甲基苯甲酰酒石酸 | CAS号68935-27-3 (+)-烟碱二对甲苯甲酰基酒石酸盐 | CAS号68935-25-1 l-nicotine di-(... | CAS号136871-75-5 (2S,3S)-2-Pheny...

D-Di(P-Methylbenzoyl)Tartaric Anhydride置于水体系中,用 甲苯 作为反应溶剂,化学反应 5.0H,以374.4G的收率获得产物d-(+)-二对甲基苯甲酰酒石酸
参考文献:一种d-对甲基二苯甲酰酒石酸的合成方法
标题:一种d-对甲基二苯甲酰酒石酸的合成方法
摘要:一种d-对甲基二苯甲酰酒石酸的合成方法,以d-酒石酸,对甲基苯甲酰氯为原料,硫酸铜为催化剂,以甲苯作为反应溶剂,化学反应制得d-对甲基二苯甲酰酒石酸酐,加等量水与甲苯水解得d-对甲基二苯甲酰酒石酸,其中溶剂甲苯,与水解步骤中水和甲苯皆可重复利用.本发明的方法工艺简单,安全易操作,工艺收率达到95%以上,同时,原料成本较低,且部分原料可回收循环利用,成品产物纯度较高,具有优异的手性拆分性能.

专利信息

专利号:US-5840915-A
优先权日:1990-01-22
标题:Process for the enatioselective synthesis of intermediates used
发明人：LEE THOMAS BING KIN; WONG GEORGE SEUNG-KIT
权利人:HOECHST MARION ROUSSEL INC
摘要:A process for the stereoselective synthesis of [R]- and [S]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-indole-3-acetonitriles comprises reacting racemic and 5-alkoxy-substituted (+/-)-1,3-dimethyloxindoles with a halogenated acetonitrile in the presence of a substituted N-benzyl cinchoninium, quinidinium, cinchonidinium, or quininium catalyst. The resulting alkylated oxindoles can be converted to primary amines by catalytic reduction in the presence of hydrogen gas. One of the primary amines, such as enantiomers of 3-(2-aminoethyl)-1,3-dihydro-1,3-dimethyl-5-methoxy-2H-indol-2-one, can be enriched by contact with a chiral tartaric acid in an amount sufficient to preferentially precipitate a salt of the chiral acid and one of the enantiomers. The product can be used in the synthesis of stereospecific forms of physostigmine and related compounds having pharmaceutical activity.

专利号:US-5274117-A
优先权日:1990-01-22
标 题:Process for the enantioselective synthesis of intermediates used in the preparation of physostigmine
发明人：LEE THOMAS BING KIN DR; WONG GEORGE S K
权利人:HOECHST ROUSSEL PHARMA
摘要:A process for the stereoselective synthesis of [R]- and [S]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-indole-3-acetonitriles comprises reacting racemic and 5-alkoxy-substituted (+/-)-1,3-dimethyloxindoles with a halogenated acetonitrile in the presence of a substituted N-benzyl cinchoninium, quinidinium, cinchonidinium, or quininium catalyst. The resulting alkylated oxindoles can be converted to primary amines by catalytic reduction in the presence of hydrogen gas. One of the primary amines, such as enantiomers of 3-(2-aminoethyl)-1,3-dihydro-1,3-dimethyl-5-methoxy-2H-indol-2-one, can be enriched by contact with a chiral tartaric acid in an amount sufficient to preferentially precipitate a salt of the chiral acid and one of the enantiomers. The product can be used in the synthesis of stereospecific forms of physostigmine and related compounds having pharmaceutical activity.

专利号:EP-0438796-B1
优先权日:1990-01-22
标题:Process for the enantioselection synthesis of alkylated oxindoles used as intermediates in the preparation of physostigmine
发明人：LEE THOMAS BING KIN DR; WONG GEORGE S K
权利人:HOECHST MARION ROUSSEL INC
摘要:A process for the stereoselective synthesis of [R]- and [S]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-indole-3-acetonitriles comprises reacting racemic and 5-alkoxy-substituted (+/-)-1,3-dimethyloxindoles with a halogenated acetonitrile in the presence of a substituted N-benzyl cinchoninium, quinidinium, cinchonidinium, or quininium catalyst. The resulting alkylated oxindoles can be converted to primary amines by catalytic reduction in the presence of hydrogen gas. One of the primary amines, such as enantiomers of 3-(2-aminoethyl)-1,3-dihydro-1,3-dimethyl-5-methoxy-2H-indol-2-one, can be enriched by contact with a chiral tartaric acid in an amount sufficient to preferentially precipitate a salt of the chiral acid and one of the enantiomers. The product can be used in the synthesis of stereospecific forms of physostigmine and related compounds having pharmaceutical activity.

专利号:EP-2589587-A1
优先权日:2011-11-04
标题:Synthesis of nitrogen substituted cyclopropanes
发明人：RASPARINI MARCELLO; TADDEI MAURIZIO; CINI ELENA; MINELLI COSIMA; TURNER NICHOLAS; HUGENTOBLER KATHARINA GLORIA
权利人:CHEMO IBERICA SA
摘要:The invention is about a new synthetic pathway for the preparation of enantiomerically pure nitrogen substituted cyclopropanes, in particular the trans- cyclopropanamine ( 1 ), a key intermediate in the synthesis of Ticagrelor:n n The invention also relates to the processes for preparing said compounds or their salts and the use of said compounds as intermediates in preparing pharmaceutically active ingredients.

专利号:US-7259263-B2
优先权日:2005-06-29
标题:Method of synthesis of azole-containing amino acids
发明人：HLASTA DENNIS J; ZIFICSAK CRAIG A
权利人:JANSSEN PHARMACEUTICA NV
摘要:The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): n nThe invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.

专利号:US-9981949-B2
优先权日:2008-12-01
标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine
发明人：AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT
权利人:OYSTER POINT PHARMA INC
摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.