"> Process for preparation of 4
    2.
    发明授权
    Process for preparation of 4"-deoxyerythromycins A and B 失效
    4“ - 脱氧红霉素A和B的制备方法

    公开(公告)号:US5760198A

    公开(公告)日:1998-06-02

    申请号:US785451

    申请日:1997-01-17

    IPC分类号: C07H17/08 C07H1/00

    CPC分类号: C07H17/08

    摘要: A process for the preparation of 4"-deoxyerythromycins, having the formula: ##STR1## wherein R is H or OH, and R.sup.1 is H or loweralkyl by treatment of the 2'-O-acetyl-4"-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H.sub.3 PO.sub.2 and an organic base in a water-miscible solvent and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.

    摘要翻译: 一种制备4'-脱氧红霉素的方法,具有下式:其中R为H或OH,R1为H或低级烷基,通过处理2'-O-乙酰基-4“ - 咪唑硫代羰基 - 红霉素 起始材料与自由基引发剂4,4'-偶氮双(4-氰基戊酸),H 3 PO 2和有机碱在水混溶性溶剂中并任选除去2'-O-乙酰基。 在优选的实施方案中,水混溶性溶剂是醇,脱氧和脱乙酰化在一个步骤中进行。

    Process for the preparation of a substituted 2,5-diamino-3-hydroxyhexane
    4.
    发明授权
    Process for the preparation of a substituted 2,5-diamino-3-hydroxyhexane 失效
    制备取代的2,5-二氨基-3-羟基己烷的方法

    公开(公告)号:US5672706A

    公开(公告)日:1997-09-30

    申请号:US633605

    申请日:1996-04-17

    CPC分类号: C07C213/00 C07C215/32

    摘要: A process is disclosed for the preparation of the substantially pure compound of the formula: ##STR1## comprising catalytic hydrogenation of a compound of the formula: ##STR2## wherein R.sub.6 and R.sub.7 are independently selected from ##STR3## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR4## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR5## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl; or an acid addition salt thereof.

    摘要翻译: 公开了用于制备基本上纯的下式化合物的方法:包括下式化合物的催化氢化:其中R6和R7独立地选自(i)其中Ra和Rb 独立地选自氢,低级烷基和苯基,R c,R d和R e独立地选自氢,低级烷基,三氟甲基,烷氧基,卤素和苯基; (ii)其中萘基环是未取代的或被一个,两个或三个独立地选自低级烷基,三氟甲基,烷氧基和卤素的取代基取代; 或者R 6和R 7与它们所键合的氮原子一起是其中R f,R g,Rh和R 1独立地选自氢,低级烷基,烷氧基,卤素和三氟甲基; 或其酸加成盐。