Back to results
US 10,501,403 B2Granted
Method for preparation of (S)-N1-(2-aminoethyl)-3-(4-alkoxyphenyl)propane-1,2-diamine trihydrochloride
AssigneeSt Pharm Co., Ltd.
InventorsYeong Hun Kim, Hyun Woo Baek, Hyeon Jin Lee, Sang Kyu Kang, Sun Ki Chang, Geun Jho Lim
Life of this patent
Estimating the term…
Abstract
The present invention relates to a novel method for preparing (S)—N1-(2-aminoethyl)-3-(4-alkoxyphenyl)propane-1,2-diamine trihydrochloride.
Claims20
A method for preparing (S)—N1-(2-aminoethyl)-3-(4-alkoxyphenyl)propane-1,2-diamine trihydrochloride, comprising the following steps:
- (1) preparing a compound of Formula 2 by Grignard coupling of a compound of Formula 1;
- (2) preparing a compound of Formula 3 by azide substitution of the compound of Formula 2 in a reaction with sodium azide;
- (3) preparing an aziridine derivative of Formula 4 having an amino group protected by an amino-protecting group by cyclization of the compound of Formula 3 using triphenylphosphine;
- (4) preparing a compound of Formula 5 by ring opening of the compound of Formula 4;
- (5) preparing a compound of Formula 6 by a reaction for removing the amino-protecting group of the compound of Formula 5:
- wherein X is bromo or chloro, and
- R is C1-6 alkyl.
4 more elements
Dependencies are inferred from the claim text.