专利号:US-9994602-B2 优先权日:2010-12-27 标 题 :Spiroannulated nucleosides and process for the preparation thereof 发明人:CHEPURI VENKATA RAMANA; DUSHING MANGESH PANDURANG 权利人:COUNCIL SCIENT IND RES 摘要:We claim a simple strategy for the synthesis of a collection of C(3′)-spirodihydroisobenzo-furannulated and C(3′)-spirodihydroisobenzo-furannulated nucleosides featuring a [2+2+2]-cyclotrimerization as the key reaction. The cyclotrimerization reactions are facile with the unprotected nucleosides having a diyne unit. When both alkynes of the diyne are terminal, the regioselectivity is poor. However, when one of the terminal alkynes is additionally substituted, the cyclotrimerizations are highly diastereoselective. Since the key bicycloannulation is the final step, this strategy provides flexibility in terms of the alkynes and is thus amenable for the synthesis of a focussed small molecule library.
专利号:US-6995001-B2 优先权日:2002-10-03 标题 :Processing for preparing monoprotected diols from symmetric diols 发明人:GU JIANXIN; RUPPEN MARK EDWARD 权利人:WYETH CORP 摘要:This invention provides a two-step enzymatic process for the synthesis of monoprotected diols from symmetric diols.