A STUDY ON ANTITUMOR CHEMOTHERAPEUTIC AGENTS——SYNTHESIS OF HEXOESTROL DIBROMOACETATE (HL-286)

Hexoestrol dibromoacetate (HL-286) -meso 3,4-bis- (P-bromoacetoxyphenyl)-n-hexane (Ⅴ), a novel compound of non-steroid oestrogen was synthesized. According to known methods, compounds Ⅱ～Ⅳ was synthesized.Compound Ⅴ was synthesized from Ⅳ by condensation with bromoacetyl bromide in 8.2% overall yield. This compound was shown to have potent inhibitory action on mice tumour S-180,S-37 and U-14.Preliminary clinical trials on 78 patients with prostate cancer showed promising results. Hexoestrol dibromoacetate has been recommended for clinical.