반응식
CC1NC(=O)C2C(=CC3CCC(N([C:20]4[CH:21]=[CH:22][C:23]([C:26]([OH:28])=[O:27])=[N:24][CH:25]=4)CC#C)C=3C=2)N=1.FC(F)(F)C(O[C:34]1[C:39]([F:40])=[C:38]([F:41])[C:37]([F:42])=[C:36]([F:43])[C:35]=1[F:44])=O>>[N:24]1[CH:25]=[CH:20][CH:21]=[CH:22][C:23]=1[C:26]([O:28][C:34]1[C:35]([F:44])=[C:36]([F:43])[C:37]([F:42])=[C:38]([F:41])[C:39]=1[F:40])=[O:27]참가 물질
실험 절차
Using analogous procedures to those described in Example 12, 5-[N-((6RS)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]pyridine-2-carboxylic acid was reacted with pentafluorophenyl trifluoroacetate to give the pentafluorophenyl pyridine-2-carboxylate which was in turn reacted with diethyl L-glutamate to give diethyl N-{5-[N-((6RS)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]pyridyl-2-carbonyl}-L-glutamate in 93% yield which was in turn hydrolysed with aqueous sodium hydroxide solution to give N-{5-[N-((6RS)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]pyridyl-2-carbonyl}-L-glutamic acid in 77% yield, m.p. 199°-201° C.;
출처 및 근거
- ORD 기록
- ord-4380aa0e2b2c428bbcb86bcdc55a47ff
- 출처 데이터셋
- uspto-grants-1998_08
- 특허 번호
- US05789417
연결된 노트
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