benzyl (2S,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1~2,6~.0~7,28~.0~8,13~.0~15,19~.0~20,27~.0~21,26~]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl(methyl)carbamate -Drug Synthesis Database

【结构式】

【分子编号】56662

【品名】benzyl (2S,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1~2,6~.0~7,28~.0~8,13~.0~15,19~.0~20,27~.0~21,26~]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl(methyl)carbamate

【CA登记号】

【分子式】C₃₆H₃₂N₄O₅

【分子量】600.67404

【元素组成】C 71.99% H 5.37% N 9.33% O 13.32%

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)

The reaction of staurosporine (I) with benzyl chloroformate (II) by means of NaHCO3 in acetone gives the N-protected compound (II), which is oxidized with lead tetraacetate in HOAc to yield the hydroxy compound (III). Finally, this compound is deprotected by hydrogenation with H2 over Pd/C in DMF to obtain the target hydroxy staurosporine.

参考文献中间体

合成目标

【1】 Murakata, C.; Sato, A.; Kasai, M.; Morimoto, M.; Akinaga, S. (Kyowa Hakko Kogyo Co., Ltd.); Staurosporin derivatives. EP 0383919; JP 2766360B2; WO 8907105 .

中间体序号	中间体编号	品名	分子式	供应商	用于合成
(I)	52822	(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1~2,6~.0~7,28~.0~8,13~.0~15,19~.0~20,27~.0~21,26~]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	C₂₈H₂₆N₄O₃	详情	详情
(II)	56662	benzyl (2S,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1~2,6~.0~7,28~.0~8,13~.0~15,19~.0~20,27~.0~21,26~]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl(methyl)carbamate	C₃₆H₃₂N₄O₅	详情	详情
(III)	56663	benzyl (2S,4R,6R)-18-hydroxy-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1~2,6~.0~7,28~.0~8,13~.0~15,19~.0~20,27~.0~21,26~]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl(methyl)carbamate	C₃₆H₃₂N₄O₆	详情	详情

Extended Information