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    • 55. 发明授权
    • Process for the preparation of carbacyclic nucleosides, and intermediates
    • 制备碳环核苷的方法和中间体
    • US5332814A
    • 1994-07-26
    • US969631
    • 1992-10-30
    • Heinz Moser
    • Heinz Moser
    • A61K31/44A61K31/505A61K31/52A61K31/522A61P31/12C07C35/06C07D239/46C07D239/47C07D239/54C07D319/08C07D327/10C07D471/04C07D473/00C07D473/02C07D473/18C07D487/04C07F7/18C07F9/6571C07F9/6574C07D239/553
    • C07D239/47C07C35/06C07D239/54C07D319/08C07D327/10C07D471/04C07D473/00C07D487/04C07F7/184C07F9/657181C07F9/65744Y02P20/55
    • Process for the preparation of racemic compounds of the formula I ##STR1## or enantiomers thereof, in which B is the radical of a nucleic base from the series comprising purine, a purine analogue or a pyridine analogue, and R is H or a protective group R.sub.1, by reactinga) a compound of the formula II or enantiomer thereof ##STR2## with a compound of the formulae X--CO--X, X--CS--X, X--SO--X, X--SO.sub.2 --X, R.sub.2 --NCO, R.sub.3 R.sub.4 N--C(O)--R.sub.5, X.sub.2 P--R.sub.6 or X.sub.2 P(O)--R.sub.6, in which X is a leaving group, R.sub.2 is, for example, C.sub.1 -C.sub.18 alkyl, R.sub.3 and R.sub.4 are, for example, H or C.sub.1 -C.sub.18 alkyl, R.sub.5 is, for example, H or C.sub.1 -C.sub.12 alkyl, and R.sub.6 is, for example, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, to give a compound of the formula III or enantiomers thereof ##STR3## in which Y is the groups --C(O)--, --C(S)--, --SO--, --SO.sub.2 --, R.sub.2 NH--CH.dbd., R.sub.3 R.sub.4 N--CR.sub.5 .dbd., R.sub.6 P.dbd. and R.sub.6 (O)P.dbd.;b) the further reaction of the compounds of the formulae III or enantiomers thereof with a nucleic base B on its own or together with a non-nucleophilic base, or with an alkali metal salt of the nucleic base B, to give compounds of the formula IV or enantiomers thereof ##STR4## in which M is H, an alkali metal or a non-nucleophilic base, and c) the conversion of the compounds of the formulae IV into the compounds of the formulae I by elimination of the protective group R.sub.1 and of the group YOM. The reactionb) is regioselective and diastereoselective, and the compounds of the formula I are obtained in high yields and purities.
    • 制备式I的外消旋化合物(I)或其对映体的方法,其中B是包含嘌呤,嘌呤类似物或吡啶类似物的系列的核酸基团,R是H或 保护基团R1,通过使a)式II化合物或其对映异构体(II)与式X-CO-X,X-CS-X,X-SO-X,X- SO2-X,R2-NCO,R3R4N-C(O)-R5,X2P-R6或X2P(O)-R6,其中X为离去基团,R2为例如C1-C18烷基,R3和R4为 例如H或C1-C18烷基,R5为例如H或C1-C12烷基,R6为例如C1-C12烷基或C1-C12烷氧基,得到式III化合物或其对映体