CARBAZOLE derivatives inhibitors of hsp90, compositions that contain nen; use of the compounds for preparing medicines; a procedure for the preparation of compounds; Medications; and composite Synthesis Intermediates

摘要

1. Prepare a product (1), wherein het represents a 5-11-step aromatic or partially unsaturated dihydrogen or tetrahydrogen monkey or bicycle variant, which is composed of 1-4 heteroatoms selected from n or s, and can optionally be replaced by one or more same or different radicals of R1 or R'1 type; As described below, r if a group consisting of formula groups is selected (2);R1 and / or R'1, same or different, consisting of H, halogenation, CF3, nitrate, cyanogen, tar, hydrogen, mercato, ammonia, leasing, diaklamino, Alcoy, fenilalcoxi, asphalt, free carbon Boxi or disinfected by radicals: asphalt, carboxida, CO-NH,There are (asphalt) 2, nh-co-asphalt, sulfur amide, nh-so2-asphalt, s (o) 2-nho tar, s (O2) - n (asphalt) 2. All the radicals of tar, alcoxi and optional asphalt are replaced by one or more equal or different radicals, which are between halogen, hydroxyl, alcoxi, amino, rental and diallamino; W1, W2, W3 are independent representatives Ch o n, X represents oxygen atom or sulfur atom or radical atom: NR2, C (o),S (o) or s (o) 2; Z represents a hydrogen atom or a halogenated atom, or a radical o-r2 or a radical nh-r2, wherein R2 represents a hydrogen atom or a radical C1-6, C3-8 cyclopropyl or c3-10 isocyclopentadiode; these tar, cyclopropyl or isocyclopropyl radicals are optionally replaced by pitch, cyclopropyl or isocyclopyl. (1);Isopropylideneisopropylidene-O-co-aspha aspha acoxi; hydroxyl; oxyhydrogen; aspha aspha rental; acrylonitrile; all these radicals are tar, propoxy and optional asphalt, replaced by one: hydrogen Xi, mercato, amino, rental Mino, diaklamino, co2quilo, nhoco2quilo, azeidino, oxetano, pirrolidino, tetrahydrofuran, 1. Piperidino, tetrahydropirano, piperazino, morfolino, homeperidino, homepedazine o quinuclidino; all of these radicals, all of which are periodic, cyclopropyl, isomerized and isomerized, are replaced by one or more radicals, which are the same as other radicals. They are selected from the radicals such as hidroxi, Aquilo, alcoxi, CH2OH, etc;Aminobenzene, rental products, diaklamino, co2quiro or nhuco2quil; including various possible ceramic and isomerized, racemic, dwarf and isomerized forms of such formula products, as well as addictive salts containing minerals and organic acids or minerals and organic bases of formula products (1),And product description (1). Item 11: as a new industrial product, intermediate formula synthetic compound (3),(4)(5)(6)(7)(8)(9) and (10) .In formula (4) Z = C (O) -OMe or C (O) -OH or OH or O-CH2-Ph or OTf, in formula (5) Z = C (O) -OMe or C (O) -OH or OH or O-CH2-Ph or OTf; in formula (7) Z = C (O) -OH or C (O) -Ome or C (O) -Oet. Products of formulas (3),(4)(5)(6)(7)(8)(9) And (10) substitutes het, R, R2, W1 and W2, which have the same meaning as formula product (1) defined in the above claim, and Z has the same meaning as in outline (1) or outline (42) above.