CAS: 5169-78-8; 3-(Dithiophen-2-Ylmethylidene)-1-Methylpiperidine

上下游产品

CAS号5166-68-7 (1-methyl-piper... | CAS号1003-09-4 2-溴噻吩 | CAS号1690-72-8 1-甲基-3-哌啶甲酸甲酯

📜(1-甲基-哌啶-3-基)-二-噻吩-2-基-甲醇置于盐酸体系中,化学反应生成 替培啶
参考文献:Okumura Et Al.,Tanabe Seiyaku Kenkyu Nenpo = Annual Report Of Gohei Tanabe Co.,1958,Vol. 3,# 2,P. 30,32
标题:Okumura Et Al.,Tanabe Seiyaku Kenkyu Nenpo = Annual Report Of Gohei Tanabe Co.,1958,Vol. 3,# 2,P. 30,32

专利信息

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-9740034-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes

专利号:JP-2000508664-A
优先权日:1996-04-22
标题:Solid-phase and combinatorial synthesis of substituted thiophenes and arrays of substituted thiophenes

专利号:EP-1021435-A1
优先权日:1996-04-22
标题:Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes