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11.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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12.发明申请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-甲基-5-（3-氧代丙基）四氢呋喃-2-基）丙醛衍生物的方法及其有用的中间体公开(公告)号：US20150073157A1
公开(公告)日：2015-03-12
申请号：US14365168
申请日：2012-12-14
IPC分类号： C07D307/28 , C07D493/10 , C07D493/08 , C07D493/04
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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13.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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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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公开(公告)号：US09758464B2
公开(公告)日：2017-09-12
申请号：US15313226
申请日：2015-04-10
发明人： Robert W. Jordan , Craig Dixon , Boris Gorin
IPC分类号： C07C67/08
CPC分类号： C07C67/08 , C07C2103/98 , C07C2603/98 , C07C69/533 , C07C67/29
摘要： Disclosed is a continuous process for the preparation of ingenol-3-mebutate by reaction, in solution, of ingenol or ingenol anion and angelic anhydride or an equivalent angelylating agent. The continuous flow process is preferably performed in the presence of a base such as lithium hexamethyl disilazane (LiHMDS) and/or an activating agent such as dicyclohexylcarbodiimide (DCC). Also disclosed is a process for recycling the other reaction products obtained in the continuous process for preparation of ingenol-3-mebutate for formation of ingenol, which can then be recycled to form ingenol-3-mebutate.
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公开(公告)号：US20170190652A1
公开(公告)日：2017-07-06
申请号：US15313226
申请日：2015-04-10
发明人： Robert W. Jordan , Craig Dixon , Boris Gorin
IPC分类号： C07C67/08
CPC分类号： C07C67/08 , C07C2103/98 , C07C2603/98 , C07C69/533 , C07C67/29
摘要： Disclosed is a continuous process for the preparation of ingenol-3-mebutate by reaction, in solution, of ingenol or ingenol anion and angelic anhydride or an equivalent angelylating agent. The continuous flow process is preferably performed in the presence of a base such as lithium hexamethyl disilazane (LiHMDS) and/or an activating agent such as dicyclohexylcarbodiimide (DCC). Also disclosed is a process for recycling the other reaction products obtained in the continuous process for preparation of ingenol-3-mebutate for formation of ingenol, which can then be recycled to form ingenol-3-mebutate.
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公开(公告)号：US09650397B2
公开(公告)日：2017-05-16
申请号：US14890127
申请日：2014-05-09
IPC分类号： C07D307/28 , C07D493/04 , C07F7/08 , C07D493/22 , C07D307/32
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.
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18.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：US20160031900A1
公开(公告)日：2016-02-04
申请号：US14882845
申请日：2015-10-14
IPC分类号： C07D493/22 , C07D493/04
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.
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20.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：US09174956B2
公开(公告)日：2015-11-03
申请号：US14365168
申请日：2012-12-14
IPC分类号： C07D493/04 , C07D493/08 , C07D493/10 , 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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