专利 已注册

PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE

专利「PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE」由 NICOX S.A 持有,当前状态为已注册,申请号 P/729。LaoBiz 老商通提供老挝知识产权信息检索与企业关联查询。

Patent “PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE” is held by NICOX S.A; status: 已注册. Search Laos IP records on LaoBiz.

申请号 P/729
申请日期 2019-02-12
注册/授权日 2023-08-21
申请人 NICOX S.A
代理机构 Tilleke & Gibbins Lao Co.,Ltd
类别 C07C 201/02 · C07C 291/02 · C07C 405/00

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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
届满日
2039-02-12
国际分类
C07C 201/02 · C07C 291/02 · C07C 405/00
商品 / 服务

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  1. 提交申请
  2. 形式审查
  3. 实质审查
  4. 公开
  5. 授权

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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 HNO3 and H2SO4 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 HNO3 and H2SO4 in dichloromethane.

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