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公开(公告)号：US20130072695A1
公开(公告)日：2013-03-21
申请号：US13674718
申请日：2012-11-12
IPC分类号： C07D493/02 , C07D493/04 , C07C405/00 , C07D307/935 , C07D307/77
CPC分类号： C07D493/04 , C07C405/00 , C07C2601/08 , C07D307/935 , C07D311/94
摘要： Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
摘要翻译： 提供了可用作前列腺素类似物合成中的中间体的稠环戊烷-4-取代的3,5-二氧戊环内酯化合物。 所述化合物具有式A：其中R表示芳基如对甲氧基苯基。 该化合物可以与低级烷基铝化合物反应以打开二氧杂环戊烷环，并将内酯还原成内酯，而不会过度还原成二醇。 所得化合物可以官能化以插入目标前列腺素的化学侧基，相互依次添加所需的α侧链，然后相互独立地添加所需的ω侧链。 这些化合物和方法特别适用于制备萝卜石。
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2.发明申请SYNTHETIC PROCESS FOR PREPARATION OF MACROCYCLIC C1-KETO ANALOGS OF HALICHONDRIN B AND INTERMEDIATES USEFUL THEREIN INCLUDING INTERMEDIATES CONTAINING -SO2-(P-TOLYL) GROUPS 有权用于制备哈利金曲霉B的大分子C1-KETO类似物的合成方法及其有用的中间体，包括含有-SO2-（P-TOLYL）基团的中间体公开(公告)号：US20160137661A1
公开(公告)日：2016-05-19
申请号：US14901481
申请日：2014-05-30
发明人： Fabio E.S. SOUZA , Alena RUDOLPH , Dino ALBERICO , Robert JORDAN , Ming PAN , Boris GORIN
IPC分类号： C07D493/04 , C07D407/14 , C07D307/20 , C07D407/06
CPC分类号： C07D493/04 , C07D307/20 , C07D307/28 , C07D407/06 , C07D407/14 , C07D493/22
摘要： Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7′, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.
摘要翻译： 公开了式1化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 7，R 8，R 9，R 10，R 11，R 12和R 13如本文所公开。 还公开了制备式1化合物或其药学上可接受的盐及其中使用的中间体的方法。 式1的化合物可用于制备软骨素类似物，例如Eribulin; 还公开了其由式1化合物制备的方法。
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公开(公告)号：US20130338379A1
公开(公告)日：2013-12-19
申请号：US13970373
申请日：2013-08-19
IPC分类号： C07D493/04 , C07C59/90 , C07D311/94 , C07D307/937
CPC分类号： C07D307/937 , C07C59/90 , C07C405/00 , C07C2601/08 , C07D307/935 , C07D311/94 , C07D493/04
摘要： Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
摘要翻译： 提供了可用作前列腺素类似物合成中的中间体的稠环戊烷-4-取代的3,5-二氧戊环内酯化合物。 所述化合物具有式A：其中R表示芳基如对甲氧基苯基。 该化合物可以与低级烷基铝化合物反应以打开二氧杂环戊烷环，并将内酯还原成内酯，而不会过度还原成二醇。 所得到的化合物可以被官能化以插入目标前列腺素的化学侧基，相加和独立地添加所需的α侧链，然后添加所需的ω-侧链。 这些化合物和方法特别适用于制备萝卜石。
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