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2. 发明授权

US3923785A (R)-3-(2-deoxy-{62 -D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo{8 4,5-d{9 {8 1,3{9 diazepin-8-ol 失效
标题翻译：（R）-3-（2-脱氧 - {62 -D-赤式 - 呋喃戊糖基）-3,6,7,8-四氢咪唑并[8,4-d {9 {8,33,9-二氮杂-8- ol
公开(公告)号：US3923785A
公开(公告)日：1975-12-02
申请号：US46282674
申请日：1974-04-22
申请人： PARKE DAVIS & CO
发明人： RYDER ALBERT , DION HENRY W , WOO PETER W , HOWELLS JOHN D
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P27/02 , A61P31/12 , C07H19/052 , C07H19/20 , C07H19/23 , C12P1/06 , C12P19/38 , C12P19/40 , C12R1/48 , C07H19/16
CPC分类号： C12P19/40 , C07H19/052 , C12P19/38 , Y10S435/888
摘要： Essentially pure (R)-3-(2-deoxy- Beta -D-erythropentofuranosyl)-3,6,7,8-tetrahydroimidazo(4,5-d)(1,3)-diazepin-8ol and the process for the production of (R)-3-(2-deoxy- Beta -Derythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo(4,5d)(1,3)diazepin-8-ol by inoculating an aqueous nutrient medium, preferably containing sources of assimilable carbon and nitrogen and added inorganic salt and having a pH between about 6 and 8, with a (R)-3-(2-deoxy- Beta -D-erythro-pentofuranosyl)-3,6,7,8tetrahydroimidazo(4,5-d)(1,3)diazepin-8-ol producing strain of Streptomyces antibioticus, such as the strain corresponding to NRRL 3238, conducting a fermentation under aseptic aerobic conditions at a temperature between about 20 and 45*C. until a substantial quantity of (R)-3-(2-deoxy- Beta -D-erythropentofuranosyl)-3,6,7,8-tetrahydroimidazo-(4,5-d)(1,3)diazepin-8ol is formed, and isolating the desired product from the fermentation mixture are disclosed. The (R)-3-(2-deoxy- Beta -Derythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo(4,5d)(1,3)diazepin-8-ol potentiates the activity of 9-( Beta -Darabinofuranosyl)adenine as an antiviral agent that is active in vitro and in vivo against DNA viruses such as herpes and vaccinia viruses.
摘要翻译：基本上纯的（R）-3-（2-脱氧-β-红 - 戊呋喃糖基）-3,6,7,8-四氢咪唑并[4,5-d] [1,3] 和（R）-3-（2-脱氧-β-D-赤型 - 呋喃戊糖基）-3,6,7,8-四氢咪唑并[4,5-d] [1,3]二氮杂的制备方法通过将（R）-3-（2-脱氧-β-D-吡喃葡萄糖）接种水性营养培养基，优选含有可同化碳和氮的来源并加入无机盐并具有约6至8的pH值的水性营养培养基，赤 - 呋喃鸟糖基）-3,6,7,8-四氢咪唑并[4,5-d] [1,3]二氮杂异恶唑生产菌Streptomyces抗生素，如对应于NRRL 3238的菌株，进行发酵在无菌需氧条件下，在约20至45℃的温度下，直到大量的（R）-3-（2-脱氧-β-D-赤型 - 戊呋喃糖基）-3,6,7,8-四氢咪唑并 - [4,5-d] [1,3]二氮杂针8-醇，并且从所述发酵混合物中分离所需产物。（R）-3-（2-脱氧-β-红 - 戊呋喃糖基）-3,6,7,8-四氢咪唑并[4,5-d] [1,3]二氮杂-8-氮醇将 9-（β-D-阿糖呋喃糖基）腺嘌呤作为抗体，在体外和体内对DNA病毒如疱疹和痘苗病毒有活性的抗病毒剂的活性。

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