| 摘要 |
<p>1327607 Steroid glycoside orthocarbonates FARBWERKE HOECHST AG 3 Dec 1970 [6 Dec 1969] 57481/70 Heading C2U The invention comprises the cyclic di-R orthocarbonates of 3 - glycosyloxy - 14# - hydroxy steroids of the 20(22)-cardenolide and 20,22- bufadienolide series, wherein each R is independently a saturated or unsaturated aliphatic hydrocarbon radical (e.g. Me, Et, Pr, Bu, pentyl, hexyl, heptyl, octyl, nonyl, decyl, allyl, propargyl). The glycosyl radical may be a monoside, bioside or trioside. Preparation of the above is by "acid"- catalysed reaction of C(OR) 4 with an appropriate free glycoside containing a cis-vicinal diol grouping. The catalyst may be an inorganic or organic acid or pyridine hydrochloride, phosphorus oxychloride or boron trifluoride etherate. Specified steroid starting materials are convallatoxin, convallatoxal, helveticoside, helveticosol, deglucohellebrin, deglucohellebrol, hellebrin, proscillaridin A, scillaren A, canarigenin 3-D-digitoxoside, eromonoside, digitoxigenin 3-D-rhamnoside, digitoxin, digoxin, gitoxin,α-antiarin, gofruside and 19-carboxymethylene 5,19-lactone 3-L-rhamnoside. The novel compounds are stated to possess cardiac activity (positive inotropic) and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.</p> |
