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    • 64. 发明申请
    • INTERMEDIATES FOR OLIGONUCLEOTIDE SYNTHESIS
    • 寡核苷酸合成的中间体
    • WO1997047636A2
    • 1997-12-18
    • PCT/GB1997001490
    • 1997-06-03
    • NOVARTIS AGCOLLINGWOOD, Stephen, PaulMOSER, Heinz, ErnstALTMANN, Karl-HeinzDOUGLAS, Mark, Edward
    • NOVARTIS AG
    • C07H19/04
    • C07H19/04Y02P20/55
    • A compound of formula (I) where B is a radical of a nucleoside base, R is hydrogen or a hydroxy-protecting group, R is hydrogen, hydroxy or a 2' nucleoside-modifying atom or group, R is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, and Z is halogen or a group of formula (II) where R and R are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, or R is said group and R is hydrogen, or R and R together with the nitrogen atom to which they are attached denote a five- to thirteen-membered heterocyclic ring, or Z is a group of formula (III): Nuc-O-, where Nuc is the residue of a natural or synthetic nucleoside or oligonucleotide after removal of a 5'-hydroxyl group therefrom attached through a 5' methylene thereof to the indicated oxygen atom.
    • 式(I)的化合物,其中B 1是核苷碱基,R 1是氢或羟基保护基,R 2是氢,羟基或2'核苷修饰原子或 基团,R 3是未取代或取代的C1至C10烷基,C2至C10烯基,C4至C10环烷基烷基,C6至C10芳基或C7至C13芳烷基,Z为卤素或式(II) R 4和R 5各自独立地为未取代或取代的C 1至C 10烷基,C 2至C 10烯基,C 4至C 10环烷基烷基,C 6至C 10芳基或C 7至C 13芳烷基,或R 4为所述基团 和R 5是氢,或者R 4和R 5与它们所连接的氮原子一起表示5至13元杂环,或Z是式(III)的基团: Nuc-O-,其中Nuc是去除通过其5'亚甲基连接到指定氧原子上的5'-羟基后天然或合成核苷或寡核苷酸的残基。
    • 67. 发明申请
    • PROCESS FOR THE PREPARATION OF HYDRAZINE DERIVATIVES USEFUL AS INTERMEDIATES FOR THE PREPARATION OF PEPTIDE ANALOGUES
    • 制备氢化衍生物的方法有助于制备肽类似物的中间体
    • WO1997046514A1
    • 1997-12-11
    • PCT/EP1997002604
    • 1997-05-22
    • NOVARTIS AG
    • NOVARTIS AGFÄSSLER, AlexanderBOLD, GuidoCAPRARO, Hans-GeorgSTEINER, Heinz
    • C07C241/02
    • C07D213/42C07B2200/07C07C253/16C07C255/44C07C281/02C07C281/04C07D213/54C07D213/55C07D257/04C07D277/30Y02P20/55
    • The invention relates to a novel process for the preparation of compounds of formula (I) wherein R1 is hydrogen or a suitable amino-protecting group, R2 is unsubstituted or substituted alkyl, R3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl, R4, independently of R1, is hydrogen or a suitable amino-protecting group and m is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds. The precursor is an oxo compound, which is in turn prepared by hydrogenation with a suitable complex hydride or with hydrogen in the presence of a suitable catalyst and acyl migration starting from a hydrazone, which is in turn preferably prepared from a nitrile via an imino compound by means of hydrogenation and reaction with a hydrazine derivative, which is prepared from an aldehyde by reaction with a reactive derivative of a carboxylic acid in the presence of a cyanide salt; and the novel intermediates required therefor.
    • 本发明涉及一种制备式(I)化合物的新方法,其中R 1为氢或适当的氨基保护基,R 2为未取代或取代的烷基,R 3为氢,芳基,杂环基,未取代或取代的烷基或未取代的 或取代的环烷基,R 4,独立地R 1为氢或适宜的氨基保护基,m为1至7的数; 并且其中可以存在其它合适的官能团保护基团; 哪些化合物是抗病毒活性的或可以用作药物活性的起始原料,特别是抗病毒化合物。 前体是氧代化合物,其又通过在合适的催化剂存在下用合适的络合氢化物或氢气氢化制备,并且从腙开始进行酰基迁移,其又优选通过亚氨基化合物由腈制备 通过氢化和与肼衍生物反应,肼衍生物通过与氰化物的存在下与羧酸的反应性衍生物反应而由醛制备; 和所需的新型中间体。