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We report a straightforward synthesis of a series of novel calcitriol analogues from vitamin D 2 with some modification of the procedures described by Calverley and Choudhry. This approach allows the large scale synthesis of a late-stage intermediate common to all the analogues of the series. This intermediate was successfully employed to synthesize a huge number of calcitriol analogues using a “click” chemistry approach.

Click chemistry approach to a series of calcitriol analogues with heterocyclic side chains