تفاعل #2028947

ord-8d48d476738b493aa9fdd287fe6c35f9

معادلة التفاعل

C[C@H]1COc2c(F)c(F)c(N)c3c(=O)c(C#N)cn1c23
5
C[C@H]1COc2c(F)c(F)c(N)c3c(=O)c(C#N)cn1c23
(S)-8-amino-9,10-difluoro-3-methyl-7-oxo-3,7-dihydro-2H-(1,4)oxazino(2,3,4-ij)quinoline-6-carbonitrile
NCCCc1cccnc1
3-(pyridine-3-yl)propan-1-amine
C[C@H]1COc2c(NCCCc3cccnc3)c(F)c(N)c3c(=O)c(C#N)cn1c23
title compound
المردود 15.1%
C[C@H]1COc2c(NCCCc3cccnc3)c(F)c(N)c3c(=O)c(C#N)cn1c23
(S)-8-amino-9-fluoro-3-methyl-7-oxo-10-(3-(pyridin-3-yl)propylamino)-3,7-dihydro-2H-(1,4)oxazino(2,3,4-ij)quinoline-6-carbonitrile
المردود 15.1%

المذيبات

ظروف التفاعل

درجة الحرارة
120°CELSIUS
الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىThe DMSO was removed under vacuo
  2. 2
    أخرىthe remaining solid was purified by preparative HPLC

الإجراء التجريبي

To a solution of 5 (30 mg, 0.108 mmol) in 5 ml of DMSO, 29.5 mg (0.216 mmol) of 3-(pyridine-3-yl)propan-1-amine were added. The reaction mixture was heated to 120° C. for 3 h. The DMSO was removed under vacuo and the remaining solid was purified by preparative HPLC to give the title compound as a yellow solid (6.4 mg, 15% yield).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US08389514B2uspto-grants-2013_03