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。
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.