US 12,344,589 B2Granted

Method for producing a 1,5-benzothiazepin compound

AssigneeElobix AB

InventorsShinya Kiguchi, Ganapati G. Bhat, Johnson M. Coutinho, Mikael Dahlstrom, Michael Lofthagen, Akinori Tatara

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Abstract

The present invention relates to a process for the preparation of a compound of formula (I) comprising: reacting a compound of formula (II) with a compound of formula (III) in the presence of a triazine compound to obtain a compound of formula (IV), and deprotecting said compound of formula (IV) to obtain the compound of formula (I). The compound of formula (I) can be prepared by the process according to the present invention in high yields and high purity. In addition, the process according to the present invention does not use a large amount of solvents or require a purification process of intermediate compounds.

Claims23

Dependent claims

A process for the preparation of a compound of formula (I):

wherein
R1 and R2 are each independently C1-4 alkyl;
R3 is C1-4 alkyl;
R4 is selected from the group consisting of hydrogen, hydroxy, halo, nitro, cyano and C1-4 alkyl;
and
R5 is selected from the group consisting of hydrogen, hydroxy, halo, nitro, cyano and C1-4 alkyl;
comprising reacting a compound of formula (II)
wherein R1, R2, R3, and R4 are each as defined above,
with a compound of formula (III) in the presence of a triazine compound:
wherein
R5 is as defined above;
and
R6 is a protecting group;
to obtain a compound of formula (IV):
wherein R1, R2, R3, R4, R5, and R6 are each as defined above,
and deprotecting said compound of formula (IV) to obtain the compound of formula (I).

13 more elements

Dependencies are inferred from the claim text.