(3S)-(-)-3-(tert-Butoxycarbonylamino)pyrrolidine → 3-(1-Aminoethyl)-1-(4-chloro-5-isoquinolinesulfonyl)azetidine

Participants

Reaction Steps

4-Chloro-5-isoquinolinesulfonyl chloride obtained in Reference Example 7 and 3-[1-(tert-butoxycarbonylamino)ethyl]azetidine obtainable from 1-(diphenylmethyl)-3-(hydroxymethyl)azetidine (Oakwood) according to the method described in WO05/080394 can be used in the method of Example 1-1, Step A instead of 4-bromo-5-isoquinolinesulfonyl chloride and (S)-3-(tert-butoxycarbonylamino)pyrrolidine, respectively, to prepare 3-[1-(tert-butoxycarbonylamino)ethyl]-1-(4-chloro-5-isoquinolinesulfonyl)azetidine, and the protective group of the obtained compound can be removed according to the method described in Example 1-1, Step B to obtain the title compound.

Provenance & Evidence