Development of a continuous flow synthesis of propranolol: tackling a competitive side reaction

被引：8

作者：

De Angelis, Sonia ^{[1
,2
]}

Celestini, Paolo ^{[3
]}

Purgatorio, Rosa ^{[1
]}

Degennaro, Leonardo ^{[1
,2
]}

Rebuzzini, Gabriele ^{[3
]}

Luisi, Renzo ^{[1
,2
]}

Carlucci, Claudia ^{[1
,2
]}

机构：

[1] Univ Bari A Moro, Dept Pharm Drug Sci, Via E Orabona 4, I-70125 Bari, Italy

[2] Flow Chem & Microreactor Technol FLAME Lab, Bari, Italy

[3] COSMA SpA, Via Colleoni 15-17, I-24040 Ciserano, BG, Italy

来源：

JOURNAL OF FLOW CHEMISTRY | 2019年 / 9卷 / 04期

关键词：

Propranolol; Tertiary amines; Ring opening; Flow chemistry; HPLC; CHEMISTRY; DERIVATIVES; EPOXIDES; AGENTS;

D O I：

10.1007/s41981-019-00047-8

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

This work reports the preparation of propranolol according to a flow process. Propranolol has been prepared paying attention to tackle the formation of the by-product tertiary amine, resulting from an additional ring opening of the starting epoxide. Remarkably, the use of catalytic amount of water resulted beneficial for the yield and purity of the desired propranolol, and to substantially reducing the amount of tertiary amine byproduct. The high concentration of the solutions allowed for a productivity of several grams/h.

引用

页码：231 / 236

页数：6

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