摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new compound, having a TNF-αproduction inhibiting activity, and useful as a TNF-αproduction inhibitor and therapeutic agent for autoimmune diseases. SOLUTION: This compound is shown by formula I (R1 is H, a lower alkyl, aryl or group shown by formula II; R2 is H, a lower alkyl, cycloalkyl or the like; R3 and R4 are each H, a lower alkyl, cycloalkylalkyl or the like; R5 is H, a lower alkyl, hydroxy or the like; R6 and R7 are each H, a lower alkyl, cycloalkylalkyl or the like; and A1 and A2 are each a lower alkylene), e.g. 1-[2-(acetylthio)ethyl]-3-[(1S)-1-benzyl-2-(dimethylamino)ethyl]-1-phe nethylurea. The compound shown by formula I is obtained, e.g. by reacting a compound shown by formula III with an amino alcohol derivative shown by formula IV in the presence of a condensation agent (e.g. 1,1'-carbonyldiimidazole), and condensing the product with a thiol derivative shown by formula V by the Mitsunobu reaction.
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