反応 #161839

ord-d7ddddeff6b44bbfb410ab52afb6f602

反応方程式

COc1ccc2c(c1)CCN(C1CCN(c3cc(C(=O)O)ncn3)CC1)C(=O)N2
6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-pyrimidine-4-carboxylic acid
C1CC2CNCC2C1.Cl
octahydrocyclopenta[c]pyrrole hydrochloride
CN(C)C(On1nnc2ccccc21)=[N+](C)C.F[B-](F)(F)F
TBTU
O=C([O-])O.[Na+]
sodium hydrogen carbonate
COc1ccc2c(c1)CCN(C1CCN(c3cc(C(=O)N4CC5CCCC5C4)ncn3)CC1)C(=O)N2
3-{1-[6-(hexahydro-cyclopenta[c]pyrrol-2-carbonyl)-pyrimidin-4-yl]-piperidin-4-yl}-7-methoxy-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-one

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    ろ過filtered
  2. 2
    その他dried

実験手順

80 mg (0.20 mmol) 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-pyrimidine-4-carboxylic acid, 40 mg (0.27 mmol) octahydrocyclopenta[c]pyrrole hydrochloride, 0.080 mL (0.57 mmol) TEA and 80 mg (0.25 mmol) TBTU were stirred in 0.9 mL DMF overnight at RT. The reaction mixture was combined with saturated sodium hydrogen carbonate solution and ice water, and the precipitated solid was suction filtered and dried.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08829006B2uspto-grants-2014_09