AMINO ACID DERIVATIVE AND ENZYMIC INHIBITOR

Japanese Patent JPH01163162

A

NEW MATERIAL:A compound expressed by formula 6 [A is R1SO2 (R1 is phenyl or naphthyl), R2CO (R2 is cyclohexyl, phenyl, etc.), etc.; B is OR3 (R3 is phenyl, naphthyl, etc.), NHR4 (R4 is phenyl, benzyl, etc.), etc.; Y is 3-aminopropyl, 3-(benzyloxycarbonylamino)propyl, etc.]. EXAMPLE:N<2>-(p-Toluenesulfonyl)-L-lysine 3-ethoxycarbonylpiperidinomethyl ketone. USE:A hemostatic agent, anti-inflammatory agent and proteolytic inhibitor having antiplasmin, antikallikrein, antitrypsin activities, etc. PREPARATION:A compound expressed by formula 1 is reacted in a solvent, such as THF or UMF, according to the reaction formula to provide a compound expressed by formula 2, which is then converted into a compound expressed by formula 3. A compound expressed by the formula H-B in an amount of 1-1.5 equiv. is subsequently added to the resultant compound expressed by formula 3 to afford a compound expressed by formula 4, which is then reacted with a solution of 4N-HCl/dioxane to provide a compound expressed by formula 5. The obtained compound expressed by formula 5 is subsequently reacted with a compound expressed by the formula A-Cl to afford the aimed compound expressed by formula 6.

OKADA YOSHIO
OKUMIYA AKIKO
TENOU NAOKI
WANAKA KEIKO
NAITO TAKETOSHI

JP32104887A

June 27, 1989

December 18, 1987

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SHOWA DENKO KK
OKAMOTO AKIYOSHI

C07C271/22; C07C67/00; C07C213/00; C07C225/06; C07C231/00; C07C233/61; C07C233/62; C07C233/76; C07C233/78; C07C235/48; C07C235/50; C07C237/24; C07C239/00; C07C311/17; C07C311/18; C07D211/30; C07D211/60; C07D213/64; C07D213/68; C12N9/99; (IPC1-7): C07C97/02; C07C103/737; C07C103/82; C07C125/065; C07C143/78; C07D211/30; C07D211/60; C07D213/64; C07D213/68; C12N9/99

Minoru Terada

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