专利号:US-2004006137-A1 优先权日:2002-06-28 标题:Asymmetric synthesis of amino-pyrrolidinones and a crystalline, free-base amino-pyrrolidinone 发明人:WALTERMIRE ROBERT E; CAMPAGNA SILVIO; SAVAGE SCOTT A; BORDAWEKAR SHAILENDRA; MADUSKUIE THOMAS P; DESIKAN SRIDHAR; ANDERSON STEPHEN R 摘要:A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below is described. n n n These compounds are useful as intermediates for MMP and TACE inhibitors. n Crystalline, free-base form of Compound J ((2R)-2-((3R)-3-amino-3-{-[(2-methyl-4-quinolinyl)methoxy]phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide): n n n which is useful as a TACE inhibitor, pharmaceutical compositions comprising the same, and methods of using the same for treating inflammatory diseases are also described.
专利号:US-2018222848-A1 优先权日:2015-08-04 标 题:Salt of Dihydrophenylglycine Methyl Ester 发明人:VAN DER DOES THOMAS; MOODY HAROLD MONRO; LI WEIDONG 权利人:DSM SINOCHEM PHARM NL BV 摘要:The present invention relates to the hemi sulfuric acid salt of methyl (R)-2-amino-2-(cyclohexa-1,4-dien-1-yl)acetate, also trivially referred to as the hemi sulfuric acid salt of D-dihydrophenylglycine methyl ester, to a method for the preparation of said salt and to the use of said salt in the enzymatic synthesis of antibiotics.
专利号:US-8703996-B2 优先权日:2010-03-09 标题:Short synthesis of tolterodin, intermediates and metabolites 发明人:STERK DAMJAN 权利人:STERK DAMJAN; LEK PHARMACEUTICALS 摘要:A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.
专利号:US-2017298406-A1 优先权日:2014-09-22 标 题 :Salt of phenylglycine methyl ester 发明人:VAN DER DOES THOMAS 权利人:DSM SINOCHEM PHARM NL BV 摘要:The present invention relates to the hemi sulfuric acid salt of D-phenylglycine methyl ester, to a method for the preparation of said salt and to the use of said salt in the enzymatic synthesis of antibiotics and of D-phenylglycine methyl ester free base.
专利号:US-8044173-B2 优先权日:2005-09-13 标 题 :Asymmetric synthesis of peptides 发明人:HARWOOD LAURENCE M; YAN RAN 权利人:UNIV READING 摘要:A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR 8 , where R 8 is C 1-6 alkyl, C 6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemisation, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.
专利号:US-8039662-B2 优先权日:2007-03-09 标 题:Process for the preparation of amino acid methyl esters 发明人:MOODY HAROLD MONRO 权利人:DSM IP ASSETS BV 摘要:The present invention describes a process for the synthesis of an amino acid methyl ester comprising the following steps: (a) refluxing a reaction mixture comprising a free amino acid, methanol and a strong acid; (b) concentrating the mixture; (c) adding methanol; (d) repeating steps a-c one or more times.
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合成参考文献
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749