PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE
「PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE」对应一条老挝专利公开记录，由 NICOX S.A 于 2019-02-12 提交申请，当前状态为已注册。关键编号与类型标注为 申请号 P/729 / DIP 编号 LAP729 / 主管局代码 LA / 保护类型 Patent - PCT National Phase。时间线要点：公开/公告日 2023-08-25；授权日 2023-08-21；届满/失效参考日 2039-02-12。国际分类 / IPC 标注为 C07C 201/02、C07C 291/02、C07C 405/00。发明人 / 设计人包括 ALMIRANTE, Nicoletta。代理机构 / 代理人记载为 Tilleke & Gibbins Lao Co.,Ltd。公开摘要提示：The present invention relates to a process for preparing the hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-…。
P/729
图样
基础信息
- 类型
- 专利
- 申请号
P/729- 状态
- 已注册
- 申请人
- NICOX S.A
- 代理机构
- Tilleke & Gibbins Lao Co.,Ltd
- 申请日期
- 2019-02-12
- 注册号
P/729- 公开 / 公告日
- 2023-08-25
- 注册 / 授权日
- 2023-08-21
- 到期日
- 2039-02-12
- 保护类型
- Patent - PCT National Phase
- 公报号
- 221 · 2023-08-25
- 优先权
- FR · 18157888.1 · 2018-02-21
- 申请人地址
- NICOX S.A · Drakkar 2-Bat D, 2405 Route des Dolines- CS 10313-Sophia Antipolis, 06560 Valbonne, France · FR
- 代理地址
- Tilleke & Gibbins Lao Co.,Ltd · Road, Village, District, Vientiane Capital Lao PDR · LA
- 国际分类
- C07C 201/02 · C07C 291/02 · C07C 405/00
- 商品 / 服务
- —
办理流程
根据当前状态动态标注-
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摘要
The present invention relates to a process for preparing the hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]- 3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-propen-1-yl ester of formula (I). In accordance with the present invention, the compound (I) can be efficiently prepared with high purity by coupling bimatoprost in a boronate protected form with 6-(nitrooxy)hexanoyl chloride and removing the boronate protecting group. The 6-(nitrooxy)hexanoyl chloride intermediate is prepared by ring-opening reaction of 2-caprolactone and subsequent nitration of the 6-hydroxyhexanoic acid potassium salt with a mixture of HNO 3 and H 2 SO 4 in dichloromethane.
The present invention relates to a process for preparing the hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]- 3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-propen-1-yl ester of formula (I). In accordance with the present invention, the compound (I) can be efficiently prepared with high purity by coupling bimatoprost in a boronate protected form with 6-(nitrooxy)hexanoyl chloride and removing the boronate protecting group. The 6-(nitrooxy)hexanoyl chloride intermediate is prepared by ring-opening reaction of 2-caprolactone and subsequent nitration of the 6-hydroxyhexanoic acid potassium salt with a mixture of HNO 3 and H 2 SO 4 in dichloromethane.
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