专利 已注册

PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE

Overview

The following summary describes a Laos Patent titled “PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE”, filed by NICOX S.A on 2019-02-12; current status: Registered. Identifiers include application No. P/729; DIP id LAP729; protection kind Patent - PCT National Phase. Key dates: publication 2023-08-25; grant 2023-08-21; expiry reference 2039-02-12. Classification: C07C 201/02、C07C 291/02、C07C 405/00. Inventor(s)/designer(s): ALMIRANTE, Nicoletta. Abstract hint: 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)-…. Unique application identifiers, holders and classification text are surfaced here to reduce near-duplicate IP landing pages; always verify against the competent office.

专利 老挝 DIP

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
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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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