专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
专利号:US-5973157-A 优先权日:1997-04-18 标题 :Process for the synthesis of 1,7-diarly or heteroaryl-heptane-4-ols and new synthetic intermediates 发明人:STIVANELLO MARIANO 权利人:FABBRICA ITALIANA SINTETICI SPA 摘要:This invention offers a process for the synthesis of a compound of the formula ##STR1## wherein R' is a phenyl, a substituted phenyl, a heterocyclic aromatic group, a heterocyclic aromatic substituted group, a linear or branched alkyl group, or a cycloalkyl group. n The invention also comprises the following compounds of a formula 1' and 2' as useful new synthesis intermediates. ##STR2## wherein R is a phenyl, a substituted phenyl, an alkyl, a cycloalkyl and X is Cl, Br, I, F, CH 3 SO 3 , p--CH 3 --C 6 H 4 --SO 3 .
专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-7176223-B2 优先权日:2001-09-05 标题 :Method for synthesis of 5-(3-pyridylmethylene-)imidazolidine-2,4-dione 发明人:CALLENS ROLAND 权利人:SOLVAY 摘要:Process for the synthesis of 5-(3-pyridylmethyl)imidazolidine-2,4-dione, according to which 5-(3-pyridylmethylene)imidazolidine-2,4-dione is subjected to a hydrogenation reaction.
参考文献:10.1107/s1600536811011779 摘要:Nisar M, Ali I, Tahir MN, Qayum M, Marwat IK. 4-({[(E)-Pyridin-3-yl-methyl-idene]amino}-meth-yl)cyclo-hexa-necarb-oxy-lic acid. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1058.