公开(公告)号：US4169841A

公开(公告)日：1979-10-02

申请号：US941815

申请日：1978-09-11

申请人： Robert C. Kelly

发明人： Robert C. Kelly

IPC分类号： C07C405/00 ,  C07D311/94 ,  C07D311/02

CPC分类号： C07C405/0041 ,  C07D311/94

摘要： Processes for preparing prostacyclin analogs which are 9-deoxy-6,9-epoxymethano derivatives of prostaglandin F.sub.1.alpha. -type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.

公开(公告)号：US4145414A

公开(公告)日：1979-03-20

申请号：US832965

申请日：1977-09-13

申请人： Robert C. Kelly ,  William J. Wechter

发明人： Robert C. Kelly ,  William J. Wechter

IPC分类号： C07H19/06 ,  C07H17/00 ,  A61K31/70

CPC分类号： C07H19/06 ,  Y02P20/55 ,  Y10S514/908

摘要： 5'-Esters of ara-cytidine (1-.beta.-D-arabinofuranosylcytosine) are prepared by reacting ara-cytidine with .beta.,.beta.,.beta.-trihaloethoxycarbonyl halide or other protective agency to form a protective amido group on the primary amino nitrogen of ara-cytidine and then reacting the thus-protected compound with a reagent reactive with the 5'-O-hydroxyl group, e.g., an acylating agent, to form the 5'-O-derivative. The .beta.,.beta.,.beta.-trihaloethoxycarbonyl or other protective group is then removed. Alternately, the primary amino group of ara-cytidine can be protected from acylation by protonation. The 5'-O-derivatives in their free base or salt form are characterized in that they display the property of sustained release of the compound, ara-cytidine, when administered intramuscularly or subcutaneously. Ara-cytidine is known for its anti-viral action and for its usefulness as an agent for controlling leukemias, including acute leukemia, and the sustained release property extends the usefulness of ara-cytidine for these purposes and as an immunosuppressive agent. The 5'-O-derivatives of this invention can also be administered orally.

公开(公告)号：US4094884A

公开(公告)日：1978-06-13

申请号：US784173

申请日：1977-04-04

申请人： Robert C. Kelly

发明人： Robert C. Kelly

IPC分类号： C07D309/22 ,  C07D493/02 ,  C07D493/04

CPC分类号： C07D309/22 ,  C07D307/33 ,  C07D493/02 ,  C07D493/04

摘要： The present specification provides novel intermediates and novel processes for the synthesis of Thromboxane B.sub.2 (11a-homo-11a-oxa-PGF.sub.2.alpha.), its 15-epimer, and various carboxyl derivatives thereof. In particular, there are disclosed various bicyclic tetrahydrofuran-containing lactones useful in the above processes, and corresponding acyclic lactones.

摘要翻译： 本说明书提供了用于合成血栓烷B2（11a-homa-11a-oxa-PGF2α），其15-差向异构体及其各种羧基衍生物的新型中间体和新方法。 特别地，公开了可用于上述方法的各种双环四氢呋喃内酯，以及相应的无环内酯。

公开(公告)号：US4081594A

公开(公告)日：1978-03-28

申请号：US710622

申请日：1976-08-02

申请人： Robert C. Kelly

发明人： Robert C. Kelly

IPC分类号： C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07D307/77

CPC分类号： C07D307/935 ,  C07C405/00 ,  C07D309/12 ,  Y10S514/822 ,  Y10S514/826 ,  Y10S514/87 ,  Y10S514/926 ,  Y10S514/927

摘要： Process for the total synthesis of 11,12-unsaturated prostaglandin compounds, i.e., prostaglandin C.sub.2 type compounds and analogs, and to certain novel compounds and intermediates produced thereby. The compounds produced by said process are useful as vasodepressors and antisecretory agents, and in managing cases of renal disfunction.

公开(公告)号：US3993686A

公开(公告)日：1976-11-23

申请号：US415050

申请日：1973-11-12

申请人： Robert C. Kelly

发明人： Robert C. Kelly

IPC分类号： C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/935 ,  C07D309/12 ,  C07C69/76

CPC分类号： C07D307/935 ,  C07C405/00 ,  C07D309/12 ,  Y10S514/822 ,  Y10S514/826 ,  Y10S514/87 ,  Y10S514/926 ,  Y10S514/927

摘要： Process for the total synthesis of 11,12-unsaturated prostaglandin compounds, i.e., prostaglandin C.sub.2 -type compounds and analogs, and to certain novel compounds and intermediates produced thereby. The compounds produced by said process are useful as vasodepressors and antisecretory agents, and in managing cases of renal disfunction.

摘要翻译： 完全合成11,12-不饱和前列腺素化合物即前列腺素C2型化合物和类似物的方法，以及由此产生的某些新化合物和中间体。 由所述方法制备的化合物可用作血管抑制剂和抗分泌剂，并用于治疗肾功能障碍。

公开(公告)号：US3966751A

公开(公告)日：1976-06-29

申请号：US543196

申请日：1975-01-22

申请人： Robert C. Kelly

发明人： Robert C. Kelly

IPC分类号： C07C405/00 ,  C07D263/04 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16 ,  C07D263/06

CPC分类号： C07D263/04 ,  C07C405/00 ,  C07D307/93 ,  C07D307/935 ,  C07D317/12 ,  C07D317/14 ,  C07D317/26 ,  C07D319/06 ,  C07D319/16

摘要： Oxazolidines having the formula ##SPC1##Wherein .about. indicates endo or exo attachment, but differing in their stereoisomeric configuration, prepared by reaction of the isomers of an oxo compound of the formula ##SPC2##Wherein .about. is as defined above, with d- or l-ephedrine; useful for separating optically active isomers of the oxo compound.

摘要翻译： 具有公式的恶唑烷酮，其含量不同于其内部或外部附着物，但不同于其立体配置，通过与D-或L-丙氨酸的定义相同的公式的OXO化合物的异构体反应制备; 有用的分离氧化合物的光学活性异构体。