Lonza Inc.

Gary Ryan

Felix Previdoli

Gareth J Griffiths

Aleksander Warm

Hans P Mettler

4-Amino-2-chloro-5-cyano-6-(methylthio)primidine is produced from dicyanoketene dimethyl thioacetal and cyanamide by condensation in the presence of a base and subsequent cyclization in the presence of hydrochloric acid. The dicyanoketenedimeth thioacetal is available by reaction of malononitrile, with carbon disulfide and a base and subsequent methylation with dimethyl sulfate. The reaction sequence yields the pyrimidine derivative in good yield and practically free of by-products.

Process for the production of

A process for the production of 1-(N-methanesulfonyl-N-methylaminosulfonyl)-3-(2-pyrimidyl) urea derivatives (MMSPH). In the process, methanesulfonylmethylamine (MMSA) is first converted with chlorosulfonylisocyanata (CSI) into a 1-methanesulfonyl-1-methyl-3- (N-methanesulfonyl-N-methylaminosulfonyl) urea derivative (MMMSH) and then the MMMSH is converted with a 2-aminopyridine into the end product.

A process for the production of 1-(N-methanesulfonyl-N-methylaminosulfonyl)-3-(2-pyrimidyl) urea derivatives (MMSPH). In the process, methanesulfonylmethylamine (MMSA) is first converted with chlorosulfonylisocyanate (CSI) into a 1-methanesulfonyl-1-methyl-3-(N-methanesulfonyl-N-methylaminosulfonyl) urea derivative (MMMSH) and then the MMMSH is converted with a 2-aminopyridine into the end product.

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Visp, Switzerland

Gary Ryan