1006037-59-7Relevant articles and documents
A new enantioselective synthesis of antiobesity drug lorcaserin
Ghotekar, Ganesh S.,More, Devidas A.,Nalla, Viswanadh,Muthukrishnan
, p. 16876 - 16880 (2019)
A simple and efficient enantioselective synthesis of anti-obesity drug lorcaerin starting from easily accessible 3-chlorostyrene oxide has been described for the first time employing hydrolytic kinetic resolution as a source of chirality. The protocol might also be useful in the synthesis of structural variants of lorcaserin.
Synthesis of enantiopure antiobesity drug lorcaserin
Smilovic, Ivana Gazic,Cluzeau, Jerome,Richter, Frank,Nerdinger, Sven,Schreiner, Erwin,Laus, Gerhard,Schottenberger, Herwig
, p. 2686 - 2690 (2018)
Acylation of enantiomerically pure (R)-2-(3-chlorophenyl)propan-1-amine using chloroacetyl chloride, followed by borane reduction and aluminum chloride catalyzed cyclization yielded enantiopure lorcaserin.
Novel Synthesis of Antiobesity Drug Lorcaserin Hydrochloride
Zhu, Qihua,Wang, Junwei,Bian, Xueguo,Zhang, Lingzhi,Wei, Ping,Xu, Yungen
, p. 1263 - 1267 (2015)
A novel synthesis of antiobesity drug lorcaserin hydrochloride was accomplished in six steps. N-protection of 2-(4-chlorophenyl)ethanamine with di-tert-butyl dicarbonate, N-alkylation with allyl bromide, deprotection, intramolecular Friedel-Crafts alkylation, chiral resolution with l-(+)-tartaric acid, and the final salification led to the target molecule lorcaserin hydrochloride in 23.1% overall yield with 99.9% purity and excellent enantioselectivity (>99.8% ee). This convenient and economical procedure is remarkably applicable for scale-up production.
Synthesis process of weight-reducing drug lorcaserin hydrochloride intermediate
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, (2020/04/17)
The invention discloses a synthesis process of a weight-reducing drug lorcaserin hydrochloride intermediate (compound V), which is characterized in that p-chlorophenylethylamine is used as a raw material, acetic anhydride is subjected to acylation to prot
Light-Enabled Enantiodivergence: Stereospecific Reduction of Activated Alkenes Using a Single Organocatalyst Enantiomer
Hostmann, Theresa,Molloy, John J.,Bussmann, Kathrin,Gilmour, Ryan
, p. 10164 - 10168 (2019/12/24)
Light-enabled enantiodivergence is demonstrated in which the alkene substrate configuration is manipulated (E → Z) prior to organocatalytic reduction with a chiral thiourea and Hantzsch ester. This allows stereodivergent reduction to be regulated at the substrate level with high fidelity and mitigates the need for a second, enantiomeric catalyst (up to 93:07 and 95:5 er). The synthetic utility of this strategy has been demonstrated in the synthesis of the weight-loss drug (R)-Lorcaserin (Belviq) and a potent AMPA modulator.