CAS: 859199-06-7; 1-(5-Bromo-4-Methylthiophen-2-yl)Ethanone

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2-乙酰基-4-甲基硫代苯 1-(4-Methyl-Thiophen-2-yl)-Ethanone 13679-73-7

2-乙酰基-4-甲基硫代苯置于n-溴代丁二酰亚胺(Nbs)体系中,化学反应 2.0H,以2.5 G的收率获得产物医药中间体
参考文献:一类嘧啶并杂环类化合物,制备方法和用途
标题:一类嘧啶并杂环类化合物,制备方法和用途
摘要:本发明公开了一类嘧啶并杂环类化合物,制备方法和用途,具体为一种如通式i所示的嘧啶并稠环类化合物,或其药学上可接受的盐,或其对映异构体,非对映异构体,互变异构体,扭转异构体,溶剂化物,多晶型物或前药,其制备方法及在药学上的应用,其中各基团的定义如说明书中所述.

专利信息

专利号:US-2004266796-A1
优先权日:2003-06-25
标 题:Convergent processes for the synthesis of a GARFT inhibitor containing a methyl substituted thiophene core and intermediates therefor
发明人：DOVALSANTOS ELENA; FLAHIVE ERIK JON; HALDEN BRIAN JOHN; MITCHELL MARK BRYAN; NOTZ WOLFGANG REINHARD LUDWIG; O'NEILL-SLAWECKI STACY ANN; TIAN QINGPING
权利人:AGOURON PHARMA
摘要:The invention relates to processes for the preparation of a GARFT inhibitor containing a methyl substituted thiophene core having the following structure: n n n wherein each of R 1 and R 2 are independently a hydrogen atom or a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; from an intermediate of the formula n n n wherein R 3 is a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; n Pg 1 is an amino protecting group; n R 4 is H; n or Pg 1 can optionally be taken together with R 4 and the nitrogen to which Pg 1 and R 4 are attached to form (i) an imine; or (ii) a fused or bridged bicyclic ring or a spirocyclic ring, wherein said ring is saturated and contains from 5 to 12 carbon atoms in which up to 2 carbon atoms are optionally replaced with a hetero moiety selected from O, S(O) j wherein j is an integer from 0 to 2, and —NR 8 —, provided that two O atoms, two S(O) j moieties, or an O atom and a S(O) j moiety are not attached directly to each other; n R 5 is selected from the group consisting of —C≡C— and —CHâ•?CH—; and n R 8 is independently H or C 1 -C 6 alkyl; n to form the compound of the formula (I) that is optically pure; and to processesfor preparing intermediates thereof.