Process for crystallizing a 4-azasteroid 5alpha-reductase inhibi

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546 77, C07S 7300, A61K 3158

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055853838

ABSTRACT:
By this invention, there is provided a process for producing crystalline 4,7.beta.-dimethyl-4-aza-5.alpha.-cholestan-3-one of structural formula (I) from 4,7.beta.-dimethyl-4-aza-5.alpha.-cholestan-3-one oil. ##STR1## This crystallization process of the present invention comprises crystallization of the oil optionally containing residual solvent with vigorous but controlled agitation. Preferably, this crystallization process is carried out at select and controlled temperatures. Further, 4,7.beta.-dimethyl-4-aza-5.alpha.-cholestan-3-one has been found to exist in at least two novel polymorphic nonsolvated forms, herein referred to as Form I and Form II. Form I can be prepared pure by careful control of the crystallization process.

REFERENCES:
patent: 5237064 (1993-08-01), Bakshi et al.
Helliker, Wall St. Jour. Jun. 7, 1991 pp. A1, A7.
Diani et al. Jour. Clin. Endocrin & METAB. vol. 74, No. 2, pp. 345-350 (1992).
Dunitz et al., "Disappearing Polymorphs", Accounts of Chem. Research, vol. 28, pp. 193-200 (1995).
McCauley, "Detection and Characterization of Polymorphism in the Pharmaceutical Industry", AIChE Symposium Series, Particle Design via Crystallizations, vol. 87, pp. 58-63 (1991).
McKenzie et al., "Mixing Induced Crystallization of an Aza Steroid", presented at the Engineering Foundation, Control of Particulate Processes Meeting, Alberta, Canada, May 17, 1995.
Bakshi et al, "7Beta-methyl-4-aza-cholestan-3-one (MK-386) and Related 4-Azasteroids as Selective Inhibitors of Human Type 1 5alpha-Reductase," J. Med. Chem., vol. 37, pp. 3871-3874 (1994).
Tolman et al., "4-Azasteroids as 5alpha-reductase inhibitors: Identification of 4,7beta-Dimethyl-4-aza-5alpha-cholestan-3-one (MK-386) As a Scalp Isozyme Selective Inhibitor", Proceedings of the European Medical Symposium (1994).
Schwartz et al., "Pharmacodynamics of MK-386: A Novel Inhibitor of 5alpha-Reductase Type 1", Abstract in American Society for Clinical Pharmacology and Therapeutics, vol. 57, p. 171 (1995).
List Discotherm B-Product Specification Brochure (1991).
List Discotherm-Product Specification Brochure (1994).
List CRP-Product Specification Brochure (1994).
List-Equipment and Operation Units for Thermal Processes with Highly Viscous, Crusting & Free Flowing Products-Brochure (1994).
Myerson et al., "Crystals, Crystal Growth and Nucleation" in Handbook of Industrial Crystallization, Butterworth-Heineman (1993), pp. 33-63.

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