反应 #742317

ord-462662f6b3d842a0881181b01353f15d

反应方程式

COC(=O)Cn1nc(N2CCN(c3c(F)cc4c(=O)c(C(=O)O)cn5c4c3OCN5C)CC2)ccc1=O
compound 20a
COC(=O)Cn1nc(N2CCN(c3c(F)cc4c(=O)c(C(=O)O)cn5c4c3OCN5C)CC2)ccc1=O
8-Fluoro-9-[4-(1-methoxycarbonylmethyl-6-oxo-1,6-dihydro-pyridazin-3-yl)-piperazin-1-yl]-3-methyl-6-oxo-2,3-dihydro-6H-1-oxa-3,3a-diaza-phenalene-5-carboxylic acid
CN1CCOCC1
N-methylmorpholine
COc1cccc(Cn2nc(N3CCN(c4c(F)cc5c(=O)c(C(=O)O)cn6c5c4OCN6C)CC3)ccc2=O)c1
title compound
收率 28.0%
COc1cccc(Cn2nc(N3CCN(c4c(F)cc5c(=O)c(C(=O)O)cn6c5c4OCN6C)CC3)ccc2=O)c1
8-Fluoro-9-{4-[1-(3-methoxy-benzyl)-6-oxo-1,6-dihydro-pyridazin-3-yl]-piperazin-1-yl}-3-methyl-6-oxo-2,3-dihydro-6H-1-oxa-3,3a-diaza-phenalene-5-carboxylic acid
收率 28.0%

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他25 was obtained
  2. 2
    其他The crude product was purified by T.L.C

实验过程

As described for compound 20a, 25 was obtained starting from 24 (300 mg, 0.99 mmol, 2.0 eq.), pyridine (4 mL,) N-methylmorpholine (0.2 mL, 4.0 mmol, 4.0 eq.) and TNOC (140 mg, 0.50 mmol, 1.0 eq.). The crude product was purified by T.L.C. preparative to afford the title compound (80 mg, 28%) as a yellow solid.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08071590B2uspto-grants-2011_12