| 摘要 |
Prepn. of 3-hydroxyoxetanes of formula (I) comprises (1) reacting a branched carboxylic acid of formula RCOOH (II) with an epichlorohydrin of formula (III) to give an ester of formula R-CO2-CHR10-C(OH)R9-CH2Cl (IV); (2) reacting (IV) with an ether of formula CHR1=CH-OR2 (V) in the presence of a catalyst to an ester of formula R-CO2-CHR10-C(O-CHOR2-CH2R1)R9-CH2Cl (VI); (3) hydrolysis and cyclisation of (VI) in the presence of a base to an oxetane deriv. of formula (VII); (4) deacetalisation to (I) in the presence of an acid; and (5) isolation of (I). R = branched alkyl; R1 = H or Me; R2 = 1-6 C alkyl; or R1+R2 = -(CH2)3-; R9, R10 = H or 1-4 C alkyl. Also claimed is the use of (I) to produce an oxetanyl chlorosulphonyl(hetero)arylcarboxylate ester of formula (VII), by reaction of (I) with an acid chloride of formula Q-COCl (VIII). Q = 3-chlorosulphonyl-thien-2 or 4-yl, or opt. substd. 2-chlorosulphonylpyrrol-3-yl, 3-chlorosulphonylpyrid-2 or 4-yl,chlorosulphonylphenyl or chlorosulphonylmethylphenyl. |
