Application Type
Patent
Application SubType
PCT National Phase
(10) Registration Number and Date
BNN20200062 22.05.2021
Status
Registered
(180) Expiration Date
(20) Filing Number and Date
BN N/2020/0062 12.02.2019
(40) Publication Number and Date
BN N/2020/0062
A
22.05.2021
(86) PCT Filing Number and Date
(87) PCT Publication Number and Date
(85) National Entry Date
(30) Priority Details
EP 18157888.1
21.02.2018
(51) IPC Classes
(72) Inventor
(EN) ALMIRANTE, Nicoletta
(74) Representative Name
(EN) M/S Marks & Clerk Singapore : C/O Ahmad Isa & Partners, Unit 404A-410A, 4th Floor, Wisma Jaya, Jalan Pemancha, Bandar Seri Begawan BS8811, Brunei Darussalam
(54) Title
(EN) PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE
(57) Abstract
(EN)

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 HNOand H2SO4 in dichloromethane.

(58) Citations
Document Type Date Action
Event NameDateStatus
Filing12.02.2019Filed
PCT National Phase Entry03.08.2020PCT National Phase
Registration22.05.2021Registered
Publication22.05.2021Published