| 摘要 |
Intermediates for preparing compounds exhibiting anti-histamine activity are represented by the formula (A) (A) as well as the salts, C1-6alkyl esters, C1-6haloalkyl esters, C1-6alkyl amides thereof, and the amides derived from ammonia or glycine, in which RA represents -CHO or -R1COOH, wherein R1 is a C1-7 bivalent aliphatic hydrocarbon group or a single bond, RB represents a hydrogen atom, a group OR7, wherein R7 is hydrogen or C1-4acyl, or a group R8 wherein R8 is a C1-4acyloxy, RC represents a group in which B represents a hydrogen atom, or represents wherein Q represents a leaving group or a group -NR2R3, wherein R2 and R3 are the same or different and are each hydrogen, C1-4alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six members; or RC represents -CH=CH2; or represents R4 is halogen, hydrogen, hydroxy, cyano, C1-4 acyloxy, C1-4alkoxy or C1-4alkyl optionally substituted by one to three halogen atoms; and X is -N= or -CH=; provided that: (i) when RA represents -CHO, RB represents a hydrogen atom and RC represents a group -CH2CH2NR2R3, or RB and RC together with the carbon atom to which they are both attached represent or wherein R2 and R3 are as defined above; (ii) when RA represents -R1COOH, and RB represents a hydrogen atom then RC represents a group -CH2CH2Q', or both RB and RC together with the carbon atom to which they are bound represent wherein R1, R2 and R3 are as defined above; and Q' is a leaving group; (iii) when RA represents R1COOH and RB represents OR7 then RC represents CH2CH2NR2R3, wherein R1, R2, R3 and R7 are as defined above; (iv) when RA represents R1COOH and RB represents OR7 where R7 is C1-4 acyl, RC represents CH=CH2. |
