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1.发明申请SYNTHETIC PROCESS FOR PREPARATION OF MACROCYCLIC C1-KETO ANALOGS OF HALICHONDRIN B AND INTERMEDIATES USEFUL THEREIN 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公开(公告)号：US20160152631A1
公开(公告)日：2016-06-02
申请号：US15015161
申请日：2016-02-04
发明人： Fabio E.S. SOUZA , Alena RUDOLPH , Ming PAN , Boris GORIN , Teng Ko NGOOI , Jason A. BEXRUD , Ricardo ORPRECIO , Huzaifa RANGWALA
IPC分类号： C07D493/22
CPC分类号： C07D493/22 , C07C309/04 , C07D307/20 , C07D407/14 , C07D493/04
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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2.发明申请PROCESS FOR PREPARATION OF (3R)-2,4-DI-LEAVING GROUP-3-METHYLBUT-1-ENE 有权制备（3R）-2,4-二 - 脱乙烯基-3-甲基-1-环己烯的方法公开(公告)号：US20140323744A1
公开(公告)日：2014-10-30
申请号：US14361489
申请日：2012-11-29
发明人： Fabio E.S. Souza , Huzaifa Rangwala , Boris Gorin , Ming Pan
IPC分类号： C07C17/16 , C07C21/17 , C07D407/14 , C07C309/73
CPC分类号： C07C17/16 , C07B2200/07 , C07C17/093 , C07C21/14 , C07C21/17 , C07C29/09 , C07C309/65 , C07C309/66 , C07C309/73 , C07D407/14 , C07D493/22 , C07C33/423
摘要： The specification relates to compounds and process for the preparation of a compound of formula 7, where LG is a leaving group and hal is a halide and is Cl, Br or I. The compound of formula 7 can be useful in the preparation of natural products, such as halichondrin and its derivatives.
摘要翻译： 本说明书涉及制备式7化合物的化合物和方法，其中LG是离去基团，而hal是卤化物，是Cl，Br或I.式7的化合物可用于制备天然产物 ，如软骨素及其衍生物。
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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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4.发明授权Process for preparation of 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivatives and intermediates useful thereof 有权制备3 - （（2s，5s）-4-亚甲基-5-（3-氧代丙基）四氢呋喃-2-基）丙醇衍生物的方法及其有用的中间体公开(公告)号：US09416140B2
公开(公告)日：2016-08-16
申请号：US14882845
申请日：2015-10-14
IPC分类号： C07D493/04 , C07D493/10 , C07D493/22 , C07D493/08 , C07D307/12 , C07D307/20 , C07D307/28
CPC分类号： C07D493/22 , C07D307/12 , C07D307/20 , C07D307/28 , C07D493/04 , C07D493/08 , C07D493/10 , Y02P20/55
摘要： Discloses is a process for preparation of a compound of formula 7, or a derivative thereof, wherein PG1 is an alcohol protecting group. Also, disclosed are intermediates and processes for their preparation. The compound of formula 7 can be useful in the preparation of halinchondrin analogs such as Eribulin.
摘要翻译： 公开了制备式7化合物或其衍生物的方法，其中PG1是醇保护基。 还公开了它们的制备的中间体和方法。 式7的化合物可用于制备软蛋白类似物如Eribulin。
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5.发明授权Synthetic process for preparation of macrocyclic C1-keto analogs of halichondrin B and intermediates useful therein 有权用于制备软碱蛋白B的大环C1-酮类似物的合成方法及其中有用的中间体公开(公告)号：US09278979B2
公开(公告)日：2016-03-08
申请号：US14389439
申请日：2013-03-28
发明人： Fabio E. S. Souza , Alena Rudolph , Ming Pan , Boris Gorin , Teng Ko Ngooi , Jason A. Bexrud , Ricardo Orprecio , Huzaifa Rangwala
IPC分类号： C07D493/22 , C07D407/14 , C07D493/04 , C07D307/20 , C07C309/04
CPC分类号： C07D493/22 , C07C309/04 , C07D307/20 , C07D407/14 , C07D493/04
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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6.发明申请2-((2S,3S,4R,5R)-5-((S)-3-AMINO-2-HYDROXYPROP-1-YL)-4-METHOXY-3-(PHENYLSULFONYLMETHYL)TETRAHYDROFURAN-2-YL)ACETALDEHYDE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 有权-2 - （（2S，3S，4R，5R）-5 - （（S）-3-氨基-2-羟基丙-1-炔基）-4-甲氧基-3-（苯基甲基）乙基四氢呋喃-2-基）乙酰胺衍生物 及其制备方法公开(公告)号：US20150011776A1
公开(公告)日：2015-01-08
申请号：US14369442
申请日：2012-12-24
发明人： Fabio E.S. Souza , Alena Rudolph , Ming Pan , Boris Gorin , Dino Alberico
IPC分类号： C07D307/20 , C07D413/06 , C07D405/06 , C07D493/04 , A61K31/366
CPC分类号： C07D307/20 , A61K31/366 , C07D405/06 , C07D413/06 , C07D493/04 , C07D493/22 , C07H7/02 , C07H9/02
摘要： Disclosed is a compound of formula 1, as shown below, where R1, R2, R3, R4, R5, R6 and R7 are as described herein. Also, disclosed is a process for the preparation of compounds of formula 1, and intermediates used therein. The compound of formula 1 can be useful for preparation of halichondrin analogs such as Eribulin.
摘要翻译： 公开了如下所示的式1化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所述。 还公开了制备式1化合物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如Eribulin。
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公开(公告)号：US09695187B2
公开(公告)日：2017-07-04
申请号：US15015161
申请日：2016-02-04
发明人： Fabio E. S. Souza , Alena Rudolph , Ming Pan , Boris Gorin , Teng Ko Ngooi , Jason A. Bexrud , Ricardo Orprecio , Huzaifa Rangwala
IPC分类号： C07D493/22 , C07D407/14 , C07D493/04 , C07D307/20 , C07C309/04
CPC分类号： C07D493/22 , C07C309/04 , C07D307/20 , C07D407/14 , C07D493/04
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.
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8.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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9.发明申请3-((2S,5S)-4-METHYLENE-5-(3-OXOPROPYL)TETRAHYDROFURAN-2-YL)PROPANOL DERIVATIVES, THEIR PREPARATION AND INTERMEDIATES USEFUL THEREOF 有权3 - （（2S，5S）-4-甲基-5-（3-氧代丙基）四氢呋喃-2-基）丙醛衍生物，其制备和中间体有用公开(公告)号：US20160090391A1
公开(公告)日：2016-03-31
申请号：US14890127
申请日：2014-05-09
IPC分类号： C07F7/08 , C07D307/32 , C07D493/22 , C07D307/28
CPC分类号： C07F7/0812 , C07D307/28 , C07D307/32 , C07D493/22 , Y02P20/55
摘要： Discloses is a process for preparation of a compound of formula 11, or a derivative thereof, wherein PG1 is an alcohol protecting group. Also, disclosed are intermediates and processes for their preparation. The compound of formula 11 can be useful in the preparation of halinchondrin analogs.
摘要翻译： 公开了制备式11化合物或其衍生物的方法，其中PG1是醇保护基。 还公开了它们的制备的中间体和方法。 式11的化合物可用于制备软蛋白类似物。
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10.发明授权Process for preparation of (3R)-2,4-di-leaving group-3-methylbut-1-ene 有权（3R）-2,4-二离子基-3-甲基丁-1-烯的制备方法公开(公告)号：US09181152B2
公开(公告)日：2015-11-10
申请号：US14361489
申请日：2012-11-29
发明人： Fabio E. S. Souza , Huzaifa Rangwala , Boris Gorin , Ming Pan
IPC分类号： C07C17/16 , C07C309/73 , C07D493/22 , C07C309/65 , C07C309/66 , C07C17/093 , C07C21/14 , C07C21/17 , C07C29/09 , C07D407/14
CPC分类号： C07C17/16 , C07B2200/07 , C07C17/093 , C07C21/14 , C07C21/17 , C07C29/09 , C07C309/65 , C07C309/66 , C07C309/73 , C07D407/14 , C07D493/22 , C07C33/423
摘要： The specification relates to compounds and process for the preparation of a compound of formula 7, where LG is a leaving group and hal is a halide and is Cl, Br or I. The compound of formula 7 can be useful in the preparation of natural products, such as halichondrin and its derivatives.
摘要翻译： 本说明书涉及制备式7化合物的化合物和方法，其中LG是离去基团，而hal是卤化物，是Cl，Br或I.式7的化合物可用于制备天然产物 ，如软骨素及其衍生物。
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