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1.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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2.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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3.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：US09850254B2
公开(公告)日：2017-12-26
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： C07D311/00 , C07D493/04 , C07D407/14 , C07D493/22 , C07D307/20 , C07D307/28 , 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.
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5.发明申请Crystalline derivatives of (S)-1-((2R,3R,4S,5S)-5-allyl-3-methoxy-4-(tosylmethyl)tetrahydrofuran-2-YL)-3-aminopropan-2-ol 审中-公开（S）-1 - （（2R，3R，4S，5S）-5-烯丙基-3-甲氧基-4-（甲苯磺酰基甲基）四氢呋喃-2-基）-3-氨基丙-2-醇公开(公告)号：US20170066735A1
公开(公告)日：2017-03-09
申请号：US15123310
申请日：2015-03-06
发明人： Fabio E.s. Souza , Ricardo Orprecio , Ming Pan
IPC分类号： C07D307/20
CPC分类号： C07D307/20 , C07C69/76 , C07D405/06 , C07D413/06
摘要： Disclosed are salts of 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 the salts of the compounds of formula 1, and intermediates used therein. The salts of the compound of formula 1 can be useful for preparation of halichondrin analogs such as eribulin.
摘要翻译： 公开了式1化合物的盐，如下所示，其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所述。 此外，还公开了制备式1化合物的盐及其中使用的中间体的方法。 式1化合物的盐可用于制备软骨素类似物如胡椒素。
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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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7.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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8.发明授权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-基）-4-甲氧基-3-（苯基磺酰基甲基）四氢呋喃-2-基）乙醛衍生物 并进行准备公开(公告)号：US09062020B2
公开(公告)日：2015-06-23
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： C07D493/20 , C07D307/20 , C07D493/22 , C07D493/04 , A61K31/366 , C07D405/06 , C07D413/06
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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9.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：US20150065733A1
公开(公告)日：2015-03-05
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 , C07C309/04 , C07D307/20 , C07D493/04 , C07D407/14
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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