公开(公告)号：US20180244619A1

公开(公告)日：2018-08-30

申请号：US15965289

申请日：2018-04-27

Applicant: API CORPORATION

Inventor： Jun TAKEHARA ,  Masato MURAI ,  Takashi OHTANI ,  Tomoko MAEDA ,  Tsugihiko HIDAKA

IPC: C07D211/60 ,  C07C309/66 ,  C07C233/47 ,  C07D498/08

Abstract: A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below: the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below: (wherein P represents a protecting group, R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below: (wherein R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).

公开(公告)号：US20160318867A1

公开(公告)日：2016-11-03

申请号：US15108141

申请日：2014-12-26

Applicant: API CORPORATION

Inventor： Jun TAKEHARA ,  Masato MURAI ,  Takashi OHTANI ,  Tomoko MAEDA ,  Tsugihiko HIDAKA

IPC: C07D211/60 ,  C07D498/08

CPC classification number: C07D211/60 ,  C07C233/47 ,  C07C309/66 ,  C07D498/08 ,  Y02P20/55

Abstract: A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by formula (10) below: the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below: (wherein P represents a protecting group, R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below: (wherein R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).

Abstract translation: （其中R3表示含有1至4个碳原子的烷基，A表示含有1至10个碳原子的烷基，含有6至12个碳原子的芳基，含有1至4个碳原子的烷氧基或芳烷氧基 含有7〜20个碳原子的基团）。

公开(公告)号：US20180244620A1

公开(公告)日：2018-08-30

申请号：US15965316

申请日：2018-04-27

Applicant: API CORPORATION

Inventor： Jun TAKEHARA ,  Masato MURAI ,  Takashi OHTANI ,  Tomoko MAEDA ,  Tsugihiko HIDAKA

IPC: C07D211/60 ,  C07C309/66 ,  C07C233/47 ,  C07D498/08

CPC classification number: C07D211/60 ,  C07C233/47 ,  C07C309/66 ,  C07D498/08 ,  Y02P20/55

Abstract: A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below: the method comprising the step of removing the protecting group from the hydroxyl group in a compound represented by the formula (7) below: (wherein P represents a protecting group, R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by the formula (8) below: (wherein R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).

公开(公告)号：US20160347718A1

公开(公告)日：2016-12-01

申请号：US15116861

申请日：2015-02-06

Applicant: API CORPORATION

Inventor： Naoyuki WATANABE ,  Yasumasa DEKISHIMA ,  Masaki NAGAHAMA ,  Tomoko MAEDA ,  Takashi OHTANI ,  Kosuke ITO ,  Hiroshi KAWABATA

IPC: C07D239/42 ,  C12P17/12

CPC classification number: C07D239/42 ,  C12N9/0006 ,  C12P17/12

Abstract: An object of the present invention is to provide a novel method capable of producing rosuvastatin calcium and intermediates therefor efficiently, inexpensively and with high purity. The present invention provides a method of efficiently producing rosuvastatin calcium and intermediates therefor having a high purity at an industrial scale, without using an extremely low temperature reaction or a special asymmetric catalyst.

Abstract translation: 本发明的目的是提供能够高效，低成本且高纯度地生产瑞舒伐他汀钙及其中间体的新方法。 本发明提供了在不使用极低温反应或特殊的不对称催化剂的情况下，有效地生产工业规模的高纯度的瑞舒伐他汀钙及其中间体的方法。

公开(公告)号：US20180002286A1

公开(公告)日：2018-01-04

申请号：US15705349

申请日：2017-09-15

Applicant: API CORPORATION

Inventor： Jun TAKEHARA ,  Masato MURAI ,  Takashi OHTANI ,  Tomoko MAEDA ,  Tsugihiko HIDAKA

IPC: C07D211/60 ,  C07C309/66 ,  C07C233/47 ,  C07D498/08

CPC classification number: C07D211/60 ,  C07C233/47 ,  C07C309/66 ,  C07D498/08 ,  Y02P20/55

Abstract: A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below: the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below: (wherein P represents a protecting group, R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below: (wherein R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).