PURPOSE: To provide a new carbocyclic sulfonamide derivative expressed by a specific formula, having antagonistic action on thromboxane A2, i.e., blood platelet coagulation inhibitory action and smooth muscle contractive or hypertensive inhibitory action, thus useful for preventing or treating hypertension, etc.
CONSTITUTION: This derivative is expressed by formula I [R1 is COOR11, CH2OR12 or CONR13R14 (R11 is H, a 1-20C alkyl, etc.; R12 is H, etc.; R13 and R14 are each H, a 1-4C alkyl, etc.); cyclic structure Tx is expressed by formula II (cyclic structure Ac is bicyclo[2.2.1]heptane, bicyclo[2.2.1]octane, etc.; Lc is a 1-4C alkylene; R2c is H, a 1-4C alkyl, etc.)], pref. (5Z)-6-[3-[N-(4- bromobenzenesulfonyl)-aminomethyl]bicyclo[2.2.1]heptan--2-yl]hexa-5-enoic acid. It is recommended that this derivative is obtained, for example, by Wittig reaction, etc., between an aldehyde of formula III and a phosphonium salt of formula IV (Y1 is a halogen) at -78°C to room temperature in an inert solvent such as toluene in the presence of a strong base such as potassium t-butoxide.
HAMANAKA NOBUYUKI
MIYAZAKI TORU
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