PRODUCTION OF O-SILYLATED HYDROXY-CONTAINING CYCLIC ETHER

PROBLEM TO BE SOLVED: To easily produce an O-silylated hydroxy-containing cyclic ether useful as a raw material for pharmaceuticals, etc., in one-pot at a low cost dispensing with troublesome separation procedure by successively reacting a specific OH- containing cyclic ether with a bifunctional and...

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1. Verfasser: FURUSAWA KIYOTAKA
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To easily produce an O-silylated hydroxy-containing cyclic ether useful as a raw material for pharmaceuticals, etc., in one-pot at a low cost dispensing with troublesome separation procedure by successively reacting a specific OH- containing cyclic ether with a bifunctional and monofunctional silicon compounds and reacting the product with hydrofluoric acid. SOLUTION: The objective compound of formula III (when Y1 or Y2 is hydroxymethylene, the OH group is converted to OSiR4R5R6) is produced by reacting (A) a compound of formula R2R3SiX12 (R2 and R3 are each an aromatic group or a >=3C branched aliphatic group; X1 is a residue of an acid other than hydrochloric acid) with (B) a compound of formula I (R1 is a substituent free from reactivity with the component A; Y1 and Y2 are each methylene, hydroxymethylene or R1-substituted methylene; (t) and (q) are each 0 or 1) e.g. a compound of formula II [B is a (protected) nucleic acid base]}, reacting with (C) a compound of formula R4R5R6SiX2 (R4 to R6 are each an aromatic group or an aliphatic group; X2 is an eliminable group) and finally reacting with (D) hydrofluoric acid in the presence of (E) a base.