Laboratory Synthesis Of Minoxidil

Synthesis Of Minoxidil

It can be prepared by two  different methods both of them are starting from 2,4-diamino-6-chloropyrimidine (I): 1) The oxidation of (I) with m-chloroperbenzoic acid (MCPBA) gives 6-amino-4-chloro-1,2-dihydro-1-hydroxy-2-iminopyrimidine (II), which is then condensed with  piperidine. 2) A mixture of (I), 2,4-dichlorophenol (A) and KOH was heated at 150 C to give 2,4-diamino-6-(2,4-dichlorophenoxy)pyrimidine (III), which is oxidized with m-chloroperbenzoic acid (MCPBA) in alcohol giving 6-amino-4-(2,4-dichlorophenoxy)-1,2-dihydro-1-hydroxy-2-iminopyrimidine (IV). Finally, this product is treated with piperidine at 150 C.to afford the target compound minoxidil.

REFERENCE

1. Anthony, W.C.; et al.; 6-Amino-1,2-dihydro-1-hydroxy-2-imino-4-phenoxypyrimidines. CH 495361; DE 1795837; FR 1510017; GB 1167736; US 3382247; US 3382248; US 3461461
2. Hyde, T.J.; N-Alkyl pyrrolidone-plasticized copolylactam compositions. US 3644264

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