盐酸考福辛达罗帕特的合成

Synthesis of Colforsin Daropate Hydrochloride

佛司可林经叔丁基二甲基氯硅烷保护羟基、脱乙酰基、与3-氯丙酰氯和二甲胺缩合得到（3R,4a R,5S,6S,6a S,10S,10a R,10b S）-3-乙烯基-5-（3-二甲胺基丙酰氧基）十二氢-6,10b-二羟基-3,4a,7,7,10a-五甲基-10-叔丁基二甲基硅氧基-1H-萘并[2,1-b]吡喃-1-酮,然后用乙腈水溶液重排、乙酰化、氟化四丁铵脱保护基和成盐精制得到盐酸考福辛达罗帕特,总收率12.5%。

Colforsin daropate hydrochloride was synthesized from forskolin via hydroxy protection with tert-butyldimethylsilyl chloride, deacetylation, condensation with 3-chloropropionyl chloride and dimethylamin~ to give （3R,4aR,SS,6S,6aS, 10S, 10aR, 10bS） -3-vinyl-5- （3-dimethylaminopropionyloxy） dodecahydro-6,10b-dihydroxy- 3,4a, 7,7,10a-pentamethyl- 10-tert-butyldimethylsilyloxy- 1H-naphtho [2,1 -b] pyran- 1 -one, which was subjected to the rearrangement with aqueous acetonitrile, aeetylation, deproteetion with tetrabutylammonium fluoride and salt formation with an overall yield of 12.5 %.