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    • 2. 发明授权
    • Process for preparation of intermediates of carbocyclic nucleoside
analogs
    • 制备碳环核苷类似物的中间体的方法
    • US5153352A
    • 1992-10-06
    • US570198
    • 1990-08-20
    • Daniel W. NorbeckRichard J. ParizaSteven M. HannickThomas J. Sowin
    • Daniel W. NorbeckRichard J. ParizaSteven M. HannickThomas J. Sowin
    • C07C215/42C07C271/18C07C271/20C07C271/24C07C275/50C07D213/69C07D239/46C07D239/54C07D251/16C07D253/065C07D471/04C07D473/00C07D487/04C07F7/18C07F9/6561
    • C07D213/69C07C215/42C07C271/18C07C271/20C07C271/24C07C275/50C07D239/47C07D239/54C07D251/16C07D253/065C07D471/04C07D473/00C07D487/04C07F7/1856C07F9/65616C07C2101/04
    • A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occuring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein R.sub.24 is the side chain of any of the naturally occuring amino acids, --CH.sub.1 SH, --Ch.sub.2 Cl, --Ch.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is as defined above, --CH.sub.2 CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 and R.sub.23 are as defined above, --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2, --Ch.sub.2 OPO.sub.3 H.sub.2, --OCH.sub.2 PO.sub.3 H.sub.2 and --CH.sub.2 CO.sub.2 R.sub.3 wherein R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 to C.sub.10 alkyl and R.sub.3 is hydrogen, C.sub.1 to C.sub.10 alkyl, carboxyalkyl or aminoalkyl; or a pharmaceutically acceptable salt thereof.
    • 下式的化合物:其中A是嘌呤-9-基,嘌呤-9-基的杂环等价基,嘧啶-1-基或嘧啶-1-基的杂环等价基 组; E是氢,-CH 2 OH或-OH; 并且G和D独立地选自氢,C1-C10烷基,-OH,-CH2OH,-CH2OR20,其中R20是C1-C6烷基,-CH2OC(O)R21,其中R21是C1-C10烷基,-CH2OC(O) CH(R22)(NHR23)其中R22是任何天然存在的氨基酸的侧链,R 23是氢或-C(O)CH(R 24)(NH 2),其中R 24是任何天然存在的氨基酸的侧链 氨基酸,-CH1SH,-Ch2Cl,-Ch2F,-CH2Br,-CH2I,-C(O)H,-CH2CN,-CH2N3,-CH2NR1R2,-CO2R1,-CH2CH2OH,-CH2CH2OR20,其中R20如上定义, CH 2 CH 2 OC(O)R 21,其中R 21如上所定义,-CH 2 CH 2 OC(O)CH(R 22)(NHR 23)其中R 22和R 23如上定义,-CH 2 CH 2 PO 3 H 2,-Ch 2 OPO 3 H 2,-OCH 2 PO 3 H 2和-CH 2 CO 2 R 3,其中R 1和R 2独立地 选自氢和C1至C10烷基,R3为氢,C1至C10烷基,羧基烷基或氨基烷基; 或其药学上可接受的盐。