Ethyl 4-isothiocyanatopiperidine-1-carboxylate → Ethyl 4-[[[[4-[[(4-fluorophenyl)methyl]amino]-3-pyridinyl]-amino]thioxomethyl]amino]-1-piperidinecarboxylate

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Reaction Steps

A mixture of 84.7 parts of ethyl 4-isothiocyanato-1-piperidinecarboxylate, 86.8 parts of N4 -[(4-fluorophenyl)-methyl]-3,4-pyridinediamine and 450 parts of tetrahydrofuran was stirred and refluxed for 3 hours. The reaction mixture was evaporated and the residue was crystallized from acetonitrile, yielding 90 parts (52%) of ethyl 4-[[[[4-[[(4-fluorophenyl)methyl]amino]-3-pyridinyl]-amino]thioxomethyl]amino]-1-piperidinecarboxylate; mp. 166° C. (15).

Provenance & Evidence