专利号:WO-2004020401-A1 优先权日:2002-09-02 标题 :Synthesis of sulfonamide derivatives 发明人:KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM 权利人:SYNGENE INTERNAT PRIVATE LTD; KALLIKAT JOHN; MANDAL ASHIS BARAN; GANESH SAMBASIVAM 摘要:The novel method of synthesis of sulphonamide derivatives (I), comprising reaction of alkyl-4-halophenylsulfonate with an amine. Formula (I) wherein X is halogen and R1 and R2 are independently selected from group comprising (i) C1 to C15 alkyl, straight or branched, (ii) C3 to C15 cycloalkyl, substituted or unsubstituted, (iii) C2 to C15 alkenyl, straight or branched, (iv) C2 to C15 alkynyl, straight or branched, (v) phenyl or benzyl, substituted or unsubstituted, (vi) heterocycloalkyl, substituted or unsubstituted, (vii) hydrogen, (viii) form with the nitrogen to which they are attached a 3-7 membered heterocyclic moiety such as pyrolidine, piperidine, piperazine, imidazole, pyrazole, (ix) the alkyl in i) may be attached to a moiety selected from cycloalkyl or heterocycloalkyl, substituted or unsubstituted
参考标题:Preparation Of 3,4-Substituted-5-Aminopyrazoles And 4-Substituted-2-Aminothiazoles 作者:Stepan Havel,Prashant Khirsariya,Naresh Akavaram,Kamil Paruch,Benoit Carbain |发布日期:2018.12.21 摘要:3,4-Substituted-5-Aminopyrazoles And 4-Substituted-2-Aminothiazoles Are Frequently Used Intermediates In Medicinal Chemistry And Drug Discovery Projects. We Report An Expedient Flexible Synthesis Of 3,4-Substituted-5-Aminopyrazoles (35 Examples), Based On Palladium-Mediated α-Arylation Of β-Ketonitriles With Aryl Bromides. A Library Of 4-Substituted-2-Aminothiazoles (21 Examples) Was Assembled By A