CAS: 2510-22-7; 4-Ethynylpyridine

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📜4-溴吡啶置于sodium Hydroxide,Copper(L) Iodide,(C6H5)3Pd(II)Cl,二乙胺体系中,用 甲苯,乙腈 用作溶剂,化学反应 2.0H,反应生成4-乙炔基吡啶
参考文献:合成新型mptp类似物作为潜在的单胺氧化酶b(mao-B)抑制剂.
标题:合成新型mptp类似物作为潜在的单胺氧化酶b(mao-B)抑制剂.
摘要:纹状体毒素1-甲基-4-苯基-1,2,3,6-四氢吡啶(mptp)是黄酶单胺氧化酶b(mao-B)的非常好底物和弱灭活剂.为了尝试开发新型的基于机理的mao-B灭活剂,我们合成了在n或c(4)位置带有多种官能团的mptp类似物,并研究了它们与纯化的mao-B制剂的相互作用.从牛肝中分离.选择的取代基包括烯丙基,炔丙基,乙烯基,乙炔基和环丁基,即被认为是酶产生的亲电或自由基中间体的潜在来源的官能团,其可能使该酶烷基化并使之失活.C(4)取代的化合物都没有显示出明显的酶抑制剂性能,尽管有些被证明是非常好的底物.在n-取代的mptp系列中,只有4-苯基-1-炔丙基类似物是好的抑制剂.该化合物对mao-B的时间和浓度依赖性抑制与基于机制的失活途径和目前对单胺氧化酶的催化机制相一致.这些研究的结果提供了对mao-B活性位的空间特征的进一步见解,并预测四氢吡啶环的c(4)取代基所在的区域缺少反应性亲核基团.
Doi:10.1021/jm00100A023

专利信息

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-6127515-A
优先权日:1997-11-18
标 题:Functionalized resin for the synthesis of amides and peptides
发明人：MANFRE FRANCO; VANASSE BENOIT J; LABAUDINIERE RICHARD F; MORTON GEORGE C
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a functionalized amino resin of formula ##STR1## wherein S is a solid support; R is H or alkyl; A is ##STR2## Y is OH or OCOR 1 ; and R 1 is aliphatic or aromatic which is useful for the solid phase synthesis of amides, peptides and hydroxamic acids.

专利号:US-6133409-A
优先权日:1996-12-19
标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:EP-0946478-B1
优先权日:1996-12-19
标题 :Process for the solid phase synthesis of aldehydes, ketones and hydroxamic acid compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARMA INC
摘要:This invention is directed to processes for the solid-phase synthesis of aldehydes, ketones, oximes, amines and hydroxamic acid compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-6710208-B2
优先权日:1996-12-19
标题 :Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARMA INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.