CAS: 539-48-0; 1,4-Phenylenedimethanamine

上下游产品

CAS号623-26-7 对苯二甲腈 | CAS号10406-25-4 4-氰基苯甲胺 | CAS号589-29-7 对苯二甲醇 | CAS号626-17-5 间苯二甲腈 | CAS号1220120-58-0 N-tert-butoxyca... | CAS号100-97-0 乌洛托品 | CAS号623-25-6 对二氯苄 | CAS号7325-46-4 1,4-亚苯基二乙酸 | CAS号20580-52-3 Ditert-butyl 1,... | CAS号108468-00-4 1-(N-B°C-氨基甲基)-... | CAS号25790-41-4 N,N-双(苯基甲基)-1,4-苯二甲胺 | CAS号589-29-7 对苯二甲醇 | CAS号1014-98-8 1,4-Bis(is°Cyan... | CAS号623-26-7 对苯二甲腈 | CAS号623-27-8 对苯二甲醛 | CAS号13534-24-2 [4-(aminomethyl... | CAS号28170-90-3 Benzene,1,3-bis...

对苯二甲醇置于[ruhcl(Co)(Pph3)3],氨,4,5-双二苯基膦-9,9-二甲基氧杂蒽体系中,用 2-甲基-2-丁醇 作为反应溶剂,150.0 °C,1.6 Mpa 条件下,反应 20.0H,以76%的收率获得产物1,4-苯二甲胺
参考文献:改进的氨气钌催化的胺化反应:二胺和氨基酯的合成
标题:改进的氨气钌催化的胺化反应:二胺和氨基酯的合成
摘要:二醇的金属化:伯和仲二醇与氨的第一次均相催化的金属化反应会反应生成相应的二胺.其他伯醇和仲醇(包括羟基取代的酯)也可以有效地转化为伯胺.这种原子效率高的选择性胺化方法在氨气气氛中进行,没有其他氢源.
DOI:10.1002/anie.201103199

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:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-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-5847150-A
优先权日:1996-04-24
标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles
发明人：DORWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles 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 under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-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-9961509-B1
优先权日:1998-05-21
标题:Synthesis of semi-crystalline polyphthalamides through reactive extrusion of hexamethylene terephthalamide oligomer with lower melting, semi-crystalline or amorphous polyamides
发明人：LEBOEUF CHRISTIAN; HARBOURNE DAVID ALAN
权利人:LEBOEUF CHRISTIAN; HARBOURNE DAVID ALAN
摘要:This invention relates to the synthesis of semi-crystalline polyphthalamides (i.e. containing monomeric units of terephthalic acid and hexamethylene diamine) through reactive extrusion of hexamethylene terephthalamide oligomer, or the oligomer of another 6T-rich copolymer, with lower melting semi-crystalline or amorphous polyamides. This process is particularly useful since it is centered around the use of stirred autoclaves for the synthesis of the 6T oligomer and the semi-crystalline or amorphous polyamides which are subsequently combined in a twin screw extruder equipped for devolatilization of water of reaction. It can also be used for the modification of existing semi-crystalline or amorphous polyamides (not necessarily phthalamides) with low levels of 6T.

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.