CAS: 86-12-4; 1-Methyl-N-Phenyl-N-(Thiophen-2-Ylmethyl)Piperidin-4-Amine

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CAS号108-86-1 溴苯 | CAS号100051-94-3 1-methyl-4-([2]... | CAS号765-50-4 2-氯甲基噻吩 | CAS号22261-94-5 4-苯胺-1-甲基哌啶 | CAS号6846-13-5 N-phenylthiophe...

📜2-氯甲基噻吩,4-苯胺-1-甲基哌啶置于sodium Amide,Xylene体系中,化学反应生成 西那利定
参考文献:1-Methyl-4-Amino-N'-Phenyl-N'-Thenyl-Piperidines
标题:1-Methyl-4-Amino-N'-Phenyl-N'-Thenyl-Piperidines
摘要:这项发明包括以下化合物:<;Form:0717227/iv (B)/1>; 其中r为甲基或乙基,X为2-Thenyl,5-Chloro-2-Thenyl或5-Bromo-2-Thenyl.这些化合物是通过用适当的thenyl卤化物处理1-烷基-4-苯胺基哌啶制备的;溶剂和缩合剂可能存在.示例展示了(1) 1-甲基-4-(N-苯基-N-(2-Thenyl)-氨基)-哌啶及其二盐酸盐和草酸盐的生产;(2) 1-甲基-4-[n-苯基-N-(5-氯-2-Thenyl)-氨基]-哌啶及其酒石酸盐的生产;(3) 1-甲基-4-[n-苯基-N-(5-溴-2-Thenyl)-氨基]-哌啶及其酒石酸盐的生产.这些产品是抗组胺药物.

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:US-6264962-B1
优先权日:1997-12-19
标 题:Use of cinnamic acid or of at least one of its derivatives in a cosmetic composition
发明人：BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE
权利人:OREAL
摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids. n The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.

专利号:EP-1331924-B1
优先权日:2000-10-26
标题 :Use of beta-carotene and lycopene for treating ageing symptoms via the inhibition of the expression of the metalloproteinase of type 1 of the extracellular matrix
发明人：BRETON LIONEL; BAUR MARKUS
权利人:OREAL; NESTEC SA
摘要:Intimate admixtures of at least one carotenoid having provitamin A activity and at least one carotenoid devoid of provitamin A activity are well suited for treating the undesirable cutaneous signs of skin aging, in particular the determination of the skin and/or of the mucous membranes by inhibiting the activity and/or the expression of collagenases and by increasing the synthesis of collagen.

专利号:US-6660283-B2
优先权日:1997-12-19
标 题 :Use of cinnamic acid, or of at least one of its derivatives in a cosmetic composition
发明人：BRETON LIONEL; GIRERD FLORENCE; RENAULT BEATRICE
权利人:OREAL
摘要:The invention relates to the use of cinnamic acid, or of at least one of its derivatives, in a cosmetic composition as an agent for promoting the synthesis of the skin's total lipids.The invention also relates to a cosmetic composition comprising an effective amount of cinnamic acid or of at least one of its derivatives.

专利号:US-5922335-A
优先权日:1995-05-15
标 题:Uses for ascorbyl-phosphoryl-cholesterol in topical compositions
发明人：PTCHELINTSEV DMITRI
权利人:AVON PROD INC
摘要:Novel uses of 3'-(L-ascorbyl-2-o-phosphoryl)-cholesterol, 3'-(L-ascorbyl-3-o-phosphoryl)-cholesterol, structural or functional isomers thereof and salts thereof (referred to collectively as 'APC compounds') are disclosed. Such novel uses include a method of reducing epidermal synthesis of abnormal elastin, especially epidermal synthesis of abnormal elastin that results from exposure to UV radiation. Also disclosed is a novel method of stimulating keratinocyte formation of triglycerides. In addition, a novel method of achieving antioxidant activity, both in the skin and also in topical compositions, is disclosed.