FIELD: organic synthesis. SUBSTANCE: invention provides novel cycloalkyl derivatives of formula I: (I), which can be used for preparation of pharmacologically active compounds, novel solid-phase synthesis thereof, and intermediates for preparation thereof depicted by general formulas II:
(II), IV:
(IV), and V:
(V). In formula I, P denotes solid phase selected from ceramics, glass, latex, cross-linked polystyrenes, polyacrylamides, silica gels, cellulose and resin particles; L denotes C2-C12- diol residue; R1 represents hydrogen, unsubstituted or substituted alkyl, alkenyl, alkinyl, or cycloalkyl; or R2 form together unsubstituted or substituted 4-8-membered ring; R1 and R2 represents unsubstituted or substituted C1- C10-alkyl, C3-C8-cycloalkyl, or aryl; R represents unsubstituted or substituted alkyl, alkenyl, alkinyl, or cycloalkyl; or two adjacent R radicals form together unsubstituted or substituted 3-8-membered carbocyclic or heterocyclic ring; n denotes number from 0 to 4; m number from 0 to n+2. Compounds I are prepared by reaction of compound II with compound of formula III:
(III) in presence of an Lewis acid. Compounds II are prepared from compounds V. EFFECT: increased efficiency of chemical synthesis of precursors of biologically active compounds. 5 cl, 2 dwg, 1 tbl, 7 ex
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Authors
Dates
2003-01-27—Published
1997-03-06—Filed