公开(公告)号：US20180186736A1

公开(公告)日：2018-07-05

申请号：US15739877

申请日：2016-06-29

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takashi Ouchi ,  Giho Goh ,  Sunmi Kim ,  Jinsoon Choi ,  Hunsoo Park

IPC: C07D207/36 ,  C07C253/30 ,  C07C255/28 ,  C07B31/00 ,  C07B41/06 ,  C07B61/00 ,  B01J29/08 ,  B01J23/44 ,  B01J21/04 ,  B01J8/02

CPC classification number: C07D207/36 ,  B01J8/0278 ,  B01J21/04 ,  B01J23/44 ,  B01J29/08 ,  B01J2523/67 ,  B01J2523/68 ,  B01J2523/69 ,  B01J2523/824 ,  B01J2523/828 ,  B01J2523/847 ,  C07B31/00 ,  C07B41/06 ,  C07B61/00 ,  C07C253/30 ,  C07C255/28 ,  C07C255/42 ,  C07D207/34 ,  C07D401/12

Abstract: The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.

公开(公告)号：US07087751B2

公开(公告)日：2006-08-08

申请号：US10050488

申请日：2002-01-16

Applicant: Shen-Chun Kuo ,  Janet L. Mas ,  Donald Hou

Inventor： Shen-Chun Kuo ,  Janet L. Mas ,  Donald Hou

IPC: C07D487/04 ,  C07D233/60 ,  C07D233/88

CPC classification number: C07C255/28 ,  C07D233/90 ,  C07D487/04 ,  Y02P20/55

Abstract: This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.

公开(公告)号：US08853428B2

公开(公告)日：2014-10-07

申请号：US13821318

申请日：2011-10-04

Applicant: Robert Huet ,  Jean-Michel Joerger ,  Vivien Henryon

Inventor： Robert Huet ,  Jean-Michel Joerger ,  Vivien Henryon

IPC: C07D307/00

CPC classification number: C07C391/00 ,  C07C253/16 ,  C07C319/02 ,  C07C319/14 ,  C07C319/24 ,  C07D307/33 ,  C07C323/58 ,  C07C255/28

Abstract: The invention relates to a method for preparing an amino acid, or its salts, from 2-aminobutyrolactone (2ABL), said amino acid fitting the formula I, XCH2CH2CHNH2COOH, wherein X is such that X− represents a nucleophilic ion, according to which N-carboxylation of 2-aminobutyrolactone (2ABL) is achieved with carbon dioxide, and the thereby obtained 2ABL carbamate is reactive with an XH reagent or its salts.

Abstract translation: 本发明涉及一种由2-氨基丁内酯（2ABL）制备氨基酸或其盐的方法，所述氨基酸适合式I，XCH2CH2CHNH2COOH，其中X表示X-表示亲核离子，根据该方法，N 用二氧化碳实现2-氨基丁内酯（2ABL）的羧化，由此得到的2ABL氨基甲酸酯与XH试剂或其盐反应。

公开(公告)号：US20060229456A1

公开(公告)日：2006-10-12

申请号：US11453125

申请日：2006-06-14

Applicant: Shen-Chun Kuo ,  Janet Mas ,  Daonald Hou

Inventor： Shen-Chun Kuo ,  Janet Mas ,  Daonald Hou

IPC: C07D233/28 ,  C07D233/91

CPC classification number: C07C255/28 ,  C07D233/90 ,  C07D487/04 ,  Y02P20/55

Abstract: This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.

Abstract translation: 本发明涉及一种用于合成替莫唑胺，抗肿瘤化合物和类似物的新方法，以及用于该新方法的中间体。

公开(公告)号：US20030083384A1

公开(公告)日：2003-05-01

申请号：US10224890

申请日：2002-08-19

Applicant: Bristol-Myers Squibb Company to Women First HealthCare, Inc.

Inventor： Jingyang Zhu ,  Scott T. Chadwick ,  Benjamin A. Price ,  Shannon X. Zhao ,  Carrie A. Costello ,  Purushotham Vemishetti

IPC: C07C227/26 ,  A61K031/198

CPC classification number: C07C255/29 ,  C07C227/10 ,  C07C227/16 ,  C07C227/18 ,  C07C227/22 ,  C07C227/40 ,  C07C227/42 ,  C07C253/30 ,  C07C255/28 ,  C07C229/26

Abstract: Provided are processes and synthetic intermediates useful for the preparation of null-difluoromethylornithine (DFMO) having the formula 1

Abstract translation: 提供了可用于制备具有下式的α-二氟甲基鸟氨酸（DFMO）的方法和合成中间体

公开(公告)号：US20090023919A1

公开(公告)日：2009-01-22

申请号：US12239123

申请日：2008-09-26

Applicant: Shen-Chun Kuo ,  Janet L. Mas ,  Donald Hou

Inventor： Shen-Chun Kuo ,  Janet L. Mas ,  Donald Hou

IPC: C07D257/12

CPC classification number: C07C255/28 ,  C07D233/90 ,  C07D487/04 ,  Y02P20/55

Abstract: This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.

Abstract translation: 本发明涉及一种用于合成替莫唑胺，抗肿瘤化合物和类似物的新方法，以及用于该新方法的中间体。

公开(公告)号：US20050131227A1

公开(公告)日：2005-06-16

申请号：US11040784

申请日：2005-01-21

Applicant: Shen-Chun Kuo ,  Janet Mas ,  Donald Hou

Inventor： Shen-Chun Kuo ,  Janet Mas ,  Donald Hou

IPC: A61K31/4188 ,  A61P35/00 ,  C07B51/00 ,  C07C255/28 ,  C07D233/88 ,  C07D233/90 ,  C07D487/04

CPC classification number: C07C255/28 ,  C07D233/90 ,  C07D487/04 ,  Y02P20/55

Abstract: This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.

Abstract translation: 本发明涉及一种用于合成替莫唑胺，抗肿瘤化合物和类似物的新方法，以及用于该新方法的中间体。

公开(公告)号：US06194600B1

公开(公告)日：2001-02-27

申请号：US09475265

申请日：1999-08-26

Applicant: Hans Rudolf Müller ,  Heinrich Bollinger ,  Peter Schwaninger ,  Martin Kurz

Inventor： Hans Rudolf Müller ,  Heinrich Bollinger ,  Peter Schwaninger ,  Martin Kurz

IPC: C07C25500

CPC classification number: C07C253/30 ,  C07C255/28

Abstract: With the present method, a process which can be employed industrially can be used for the first time for the direct production of aminocyanoacetamide. The method is based on the reaction of cyanoacetamide with nitrites to form nitrosocyanoacetamide at a pH of around 2 and on the subsequent catalytic hydrogenation of nitrosocyanoacetamide to form aminocyanoacetamide.

Abstract translation: 采用本发明的方法，可以在工业上应用的方法首次用于直接生产氨基氰乙酰胺。 该方法是基于氰基乙酰胺与亚硝酸盐反应形成亚硝基氰基乙酰胺，pH值约为2，随后催化氢化亚硝基氰乙酰胺，形成氨基氰乙酰胺。

公开(公告)号：US20230322669A1

公开(公告)日：2023-10-12

申请号：US18132677

申请日：2023-04-10

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takashi Ouchi ,  Giho Goh ,  Sunmi Kim ,  Jinsoon Choi ,  Hunsoo Park

IPC: C07D207/36 ,  B01J23/44 ,  C07B61/00 ,  C07C253/30 ,  C07C255/42 ,  C07D401/12 ,  C07D207/34 ,  B01J8/02 ,  B01J21/04 ,  B01J29/08 ,  C07B31/00 ,  C07B41/06 ,  C07C255/28

CPC classification number: C07D207/36 ,  B01J2523/847 ,  C07B61/00 ,  C07C253/30 ,  C07C255/42 ,  C07D401/12 ,  C07D207/34 ,  B01J8/0278 ,  B01J21/04 ,  B01J29/08 ,  C07B31/00 ,  C07B41/06 ,  C07C255/28 ,  B01J2523/67 ,  B01J2523/68 ,  B01J2523/69 ,  B01J2523/824 ,  B01J2523/828 ,  B01J23/44

Abstract: The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.

公开(公告)号：US11649206B2

公开(公告)日：2023-05-16

申请号：US17350013

申请日：2021-06-17

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takashi Ouchi ,  Giho Goh ,  Sunmi Kim ,  Jinsoon Choi ,  Hunsoo Park

IPC: C07C253/30 ,  C07D207/36 ,  B01J23/44 ,  C07B61/00 ,  C07C255/42 ,  C07D401/12 ,  C07D207/34 ,  B01J8/02 ,  B01J21/04 ,  B01J29/08 ,  C07B31/00 ,  C07B41/06 ,  C07C255/28

CPC classification number: C07D207/36 ,  B01J8/0278 ,  B01J21/04 ,  B01J23/44 ,  B01J29/08 ,  C07B31/00 ,  C07B41/06 ,  C07B61/00 ,  C07C253/30 ,  C07C255/28 ,  C07C255/42 ,  C07D207/34 ,  C07D401/12 ,  B01J2523/67 ,  B01J2523/68 ,  B01J2523/69 ,  B01J2523/824 ,  B01J2523/828 ,  B01J2523/847

Abstract: The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.