公开(公告)号：US20030055274A1

公开(公告)日：2003-03-20

申请号：US10112355

申请日：2002-03-29

申请人： G.D. Searle & Company

发明人： John S. Ng ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Joseph Wieczorek ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Ping T. Wang ,  Edward E. Yonan ,  Richard M. Weier ,  Thomas B. Kowar ,  Julio A. Baez ,  Bernhard Erb

IPC分类号： C07J001/00

CPC分类号： C12P33/10 ,  C07D301/12 ,  C07J1/0059 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0094 ,  C07J53/002 ,  C07J71/0005 ,  C07J71/0015 ,  C12P33/005

摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of formula (I) wherein: nullAnullAnull represents the group nullCHR4nullCHR5null or nullCR4nullCR5null, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy; R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; nullBnullBnull represents the group nullCHR6nullCHR7null or an alpha- or beta-oriented group (III), where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and R8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring. 1

摘要翻译： 提供了多种新的反应方案，新的工艺步骤和新的中间体，用于合成环氧麦芽糖酮和式（I）的其它化合物，其中：-AA-表示-CHR 4 -CHR 5 - 或-CR 4 = CR 5 - ，R 3，R 4和 R5独立地选自氢，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基，芳氧基; R1表示α-取代的低级烷氧基羰基或羟烷基; -BB-表示基团-CHR6-CHR7-或α取代或β-取代基团（III），其中R6和R7独立地选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基 烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基; 并且R 8和R 9独立地选自氢，羟基，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基，或者R 8和R 9一起包含碳环或杂环 结构或R8或R9与R6或R7一起包含与五环D环稠合的碳环或杂环结构。

公开(公告)号：US20040191874A1

公开(公告)日：2004-09-30

申请号：US10608101

申请日：2003-06-27

申请人： G.D. Searle & Company

发明人： John S. Ng ,  Ping T. Wang ,  Julio A. Baez ,  Chin Liu ,  Dennis K. Anderson ,  Jon P. Lawson ,  Bernhard Erb ,  Joseph Wieczorek ,  Gennaro Mucciariello ,  Fortunato Vanzanella ,  Sastry A. Kunda ,  Leo J. Letendre ,  Mark J. Pozzo ,  Yuen-Lung L. Sing ,  Edward E. Yonan

IPC分类号： C12P019/02

CPC分类号： C07J71/00 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J53/00 ,  C07J53/002 ,  C07J71/0015 ,  C12P33/005 ,  C12P33/10 ,  C12Q1/02

摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I 1 wherein: -A-A- represents the group nullCHR4nullCHR5null or CR4nullCR5nullR3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy, R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical, nullBnullBnull represents the group nullCHR6nullCHR7null or an alpha- or beta-oriented group: 2 where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and R8 and R9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.

摘要翻译： 提供了多种新的反应方案，新的方法步骤和新的中间体，用于合成环氧麦芽糖酮和式I的其它化合物，其中：-AA-表示基团-CHR 4 -CHR 5 - 或CR 4 = CR R 5，R 4和R 5独立地选自氢，卤素，羟基，低级烷基，低级烷氧基，羟烷基，烷氧基烷基，羟基羰基，氰基，芳氧基， 1>表示α-取代的低级烷氧基羰基或羟烷基，-BB-表示基团-CHR 6 -CHR 7 - 或α或β-取代基团：其中R 6和R 7 烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基，R 8和R 9独立地选自氢，卤代，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基， 氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基或R 8 nd R 9一起包含碳环或杂环结构，或R 8或R 9与R 6或R 7一起包含与五环D环稠合的碳环或杂环结构。