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【结 构 式】

【分子编号】59348

【品名】N-{(6R,9S,10R,13S,15aS,22S,24aS)-22-[4-(dimethylamino)benzyl]-6-ethyl-17-hydroxy-10,23-dimethyl-18-methylene-5,8,12,15,21,24-hexaoxo-13-phenyldocosahydro-12H-pyrido[2,1-f]pyrrolo[2,1-l][1,4,7,10,13,16]oxapentaazacyclononadecin-9-yl}-3-hydroxy-2-pyridinecarboxamide

【CA登记号】

【 分 子 式 】C46H56N8O10

【 分 子 量 】880.99856

【元素组成】C 62.71% H 6.41% N 12.72% O 18.16%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(II)

Reduction of the keto group of 5-delta-methylene pristinamycin IA (I) by means of NaBH4 in the presence of CeCl3 provided the allyl alcohol (II). Subsequent chlorination of (II) with SOCl2, furnished a mixture of compounds containing the 5-delta-(chloromethyl) (III) and the 5-gamma-chloro-5-delta-methylene (IV) derivatives. Treatment of the crude mixture with morpholine (V) in refluxing acetonitrile yielded the title 5-delta-morpholinomethyl analogue.

1 Barriere, J.C.; Bacque, E.; Puchault, G.; Dutruc-Rooset, G.; Doerflinger, G.; Berthaud, N.; Design and synthesis of RPR202868, the pristinamycin I component of RPR202868/RPR132552, a new oral streptogramin. 41st Intersci Conf Antimicrob Agents Chemother (Dec 16 2001, Chicago) 2001, Abst F-359.
2 Barriere, J.-C.; Pantel, G.; Bacqué, E.; Doerflinger, G.; Dutruc-Rosset, G. (Aventis Pharma SA); Streptogramin derivs., production thereof and compsns. containing the same. EP 1204675; FR 2796949; US 6541451; WO 0110895 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 41288   C46H54N8O10 详情 详情
(II) 59348 N-{(6R,9S,10R,13S,15aS,22S,24aS)-22-[4-(dimethylamino)benzyl]-6-ethyl-17-hydroxy-10,23-dimethyl-18-methylene-5,8,12,15,21,24-hexaoxo-13-phenyldocosahydro-12H-pyrido[2,1-f]pyrrolo[2,1-l][1,4,7,10,13,16]oxapentaazacyclononadecin-9-yl}-3-hydroxy-2-pyridinecarboxamide C46H56N8O10 详情 详情
(III) 59349 N-{(6R,9S,10R,13S,15aS,22S,24aS)-18-(chloromethyl)-22-[4-(dimethylamino)benzyl]-6-ethyl-10,23-dimethyl-5,8,12,15,21,24-hexaoxo-13-phenyl-1,2,3,5,6,7,8,9,10,13,14,15,15a,16,19,21,22,23,24,24a-icosahydro-12H-pyrido[2,1-f]pyrrolo[2,1-l][1,4,7,10,13,16]oxapentaazacyclononadecin-9-yl}-3-hydroxy-2-pyridinecarboxamide C46H55ClN8O9 详情 详情
(IV) 59350 N-{(6R,9S,10R,13S,15aS,22S,24aS)-17-chloro-22-[4-(dimethylamino)benzyl]-6-ethyl-10,23-dimethyl-18-methylene-5,8,12,15,21,24-hexaoxo-13-phenyldocosahydro-12H-pyrido[2,1-f]pyrrolo[2,1-l][1,4,7,10,13,16]oxapentaazacyclononadecin-9-yl}-3-hydroxy-2-pyridinecarboxamide C46H55ClN8O9 详情 详情
(V) 10388 Morpholine 110-91-8 C4H9NO 详情 详情
Extended Information