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公开(公告)号:US06288233B1
公开(公告)日:2001-09-11
申请号:US09667411
申请日:2000-09-21
申请人: Shen-Chun Kuo , Frank Xing Chen
发明人: Shen-Chun Kuo , Frank Xing Chen
IPC分类号: C07D22106
CPC分类号: C07D401/04 , C07D401/14 , Y02P20/55
摘要: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase. Also disclosed is a compound having the formula:
摘要翻译: 公开了一种制备下式化合物的方法:其中X 1,X 2,X 3,X 4和X 5独立地选自H,卤素,烷基,烷氧基,芳基和芳氧基,R是保护基 其中具有如下定义的具有如下定义的化合物:(a)非亲核性强碱;(b)手性氨基醇(其中R 1,R 2,R 3,X 4, ; 和(c)具有甲醛的化合物L是离去基团,R如上定义。 通过该方法制备的化合物是制备法呢基蛋白转移酶抑制剂的化合物的有用中间体。 还公开了具有下式的化合物:
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公开(公告)号:US06492519B2
公开(公告)日:2002-12-10
申请号:US09836605
申请日:2001-04-17
申请人: Marc Poirier , Yee-Shing Wong , George G. Wu
发明人: Marc Poirier , Yee-Shing Wong , George G. Wu
IPC分类号: C07D22106
CPC分类号: C07D213/79 , C07D221/16
摘要: A process is provided for preparing a compound having the formula comprising: (a) reacting a compound having the formula with an isocyanate having the formula R1NCO to produce a compound having the formula (b) optionally hydrolyzing the compound of formula (III) to form an amide having the formula (c) reacting the compound of formula (III) or the amide of formula (IV) with a compound having the formula in the presence of a strong base to produce a compound having the formula and (d) cyclizing the compound of formula (VI) to obtain the compound of formula (I), wherein R is H or Cl; M is selected from the group consisting of Li, Na, K, MgX, ZnRA, and Al(RA)2; RA is alkyl; X is halo; R1 is selected from the group consisting of alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, and heterocycloalkylalkyl; and L is a leaving group.
摘要翻译: 提供了一种制备具有以下方法的化合物的方法:(a)使具有式R1NCO的异氰酸酯的化合物与具有式(b)的化合物反应,任选地水解式(III)化合物以形成酰胺 具有式(c)使式(III)的化合物或式(IV)的酰胺与具有式的化合物存在强碱反应以产生具有下式的化合物:(d)使式(III)的化合物( VI),得到其中R为H或Cl的式(I)化合物; M选自Li,Na,K,MgX,ZnRA和Al(RA)2; RA是烷基; X是卤素; R 1选自烷基,芳基,芳烷基,杂芳基,杂芳烷基,环烷基,环烷基烷基,杂环烷基和杂环烷基烷基; 而L是离职团体。
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公开(公告)号:US06372910B1
公开(公告)日:2002-04-16
申请号:US09514609
申请日:2000-02-28
IPC分类号: C07D22106
CPC分类号: C07D221/14
摘要: A process for preparing 1,8-naphthalimide by reacting 1,8-naphthalic anhydride with ammonia in an aqueous solution under atmospheric pressure at 60 to 100° C.
摘要翻译: 在大气压下,在60〜100℃下,使1,8-萘二甲酸酐与氨在水溶液中反应制备1,8-萘二甲酰亚胺的方法。
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公开(公告)号:US06608202B1
公开(公告)日:2003-08-19
申请号:US10223799
申请日:2002-08-20
IPC分类号: C07D22106
CPC分类号: C07D221/16
摘要: In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen, and intermediates therefor from easily available starting materials by a simple route.
摘要翻译: 在一个实施方案中,本发明描述了通过简单的途径合成式III化合物,其中X是卤素,并且其中间体由容易获得的原料制备。
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公开(公告)号:US06177568B1
公开(公告)日:2001-01-23
申请号:US09277178
申请日:1999-03-26
申请人: Sang Sup Jew , Hee Soon Lee , Joon Kyum Kim , Kwang Dae Ok , Kyeong Hoi Cha , Myoung Goo Kim , Kwang Kyun Lee , Jong Min Kim , Hee Jin Kim , Jeong Mi Hah
发明人: Sang Sup Jew , Hee Soon Lee , Joon Kyum Kim , Kwang Dae Ok , Kyeong Hoi Cha , Myoung Goo Kim , Kwang Kyun Lee , Jong Min Kim , Hee Jin Kim , Jeong Mi Hah
IPC分类号: C07D22106
CPC分类号: C07D491/14 , Y02P20/55
摘要: Intermediates for the synthesis of camptothecin of the formula II wherein: R1 is —(CH2)2NR1R2, where R1 is an amino protecting group and R2 is C2-C5 alkyl, hydroxyethyl or acetoxyethyl group, and of the formula III wherein: n is 1 or 2; R3 is hydrogen or —OR4, where R4 is hydrogen, —COR5, —CONHR6 or CH2OR7, where R5 is methyl or —CH2OCH3, R6 is isopropyl, phenyl or —CH2CH2Cl, and R7 is methyl, ethyl or —CH2CH2OCH3; with the proviso that when n is 2, R3 is not hydrogen.
摘要翻译: 用于合成式II的喜树碱的中间体,其中R1为 - (CH2)2NR1R2,其中R1为氨基保护基,R2为C2-C5烷基,羟乙基或乙酰氧基乙基,式III其中n为1或2 R 3是氢或-OR 4,其中R 4是氢,-COR 5,-CONHR 6或CH 2 OR 7,其中R 5是甲基或-CH 2 OCH 3,R 6是异丙基,苯基或-CH 2 CH 2 Cl,R 7是甲基,乙基或-CH 2 CH 2 OCH 3; 条件是当n为2时,R 3不是氢。
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