A process for the preparation of alpha - difluorometil ornithine (dfmo), a procedure to isolate dihydrochloride 2 - difluorometil ornithine, an intermediary compound and a process for the preparation of a compound Agent

摘要

A procedure for the preparation of a difluorometilornitina (dfmo) of the formula (1), Realizing the procedure: (a) selectively reduce a part of a Nitrile Compound of the formula (2), where R1 is a linear or branched alkyl c1-4 and Z is (i) or (ii) - NH2 Select a part) Among the group consisting of: a rest of formula (3), where R2 is Hydrogen,C1-4 alkyl aryl or linear or branched, and a remainder formula (4), where r is alkyl or aryl alkoxy, c1-4 linear or branched; (b) to be present, Hydrolyze the part of formula (3) occurring as a result of Step (STEP (a), or the step (a) and (b) a compound of one of the later Efore Formulae (5),(6) and (7); (c) to Hydrolyze the Ester and amide (including parts of the lactam) Formulae (5), (6) and (7) to give the compound of formula (1).A procedure for the preparation of the compound of the formula (1) or a pharmaceutically acceptable Salt thereof,Understanding the procedure: (a) reacting a compound of formula (8) with acrylonitrile or 3 - halopropionitrilo to give a compound of formula (9); (b) to rent the compound with chlorodifluoromethane (9) to give the compound of formula (10); (c) to Hydrolyze the composite (10) give The Compound of formula (11); (d) to selectively reduce the compound of the formula (11) with a CataliA heterogeneous Catalyst of transition metal selected from Platinum and Palladium catalysts in the presence of an acid to give a compound of formula (1) or a Salt thereof; and (e) Hydrolyze the Ester Compound (5) with an acid to provide Compound (1). Procedure for the preparation of the compound of formula (10), described above.A procedure for Isolating dihydrochloride 2 - difluorometilornitina comprising: (a) treating a solution of 2 - difluorometilornitina and hydrochloric acid in a Tertiary alcohol with sufficient basis of alkylamine to achieve a pH of approx. 3.8 to 4.2 to form a Slurry; and (b) recovering the dihydrochloride difluorometilornitina 2 - from the slurry.A compound Agent of formula (12), where R5 has the values of Z given above.The dfmo has a large number of applications within which include substance use as a composition for inhibiting the growth of unwanted Hair, such as anti - Cancer Therapy and as anti inflammatory for its ability to disrupt Cell Metabolism in a number of types Cells.