반응 #161866

ord-8f61b31e096f47d397a24faf8efcc2bd

반응 방정식

CN(C)C(On1nnc2ccccc21)=[N+](C)C.F[B-](F)(F)F
TBTU
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
Fc1ccc2c(c1)NCC2
6-fluoro-2,3-dihydro-1H-indole
COc1ccc2c(c1)CCN(C1CCN(c3cc(C(=O)N4CCc5ccc(F)cc54)ncn3)CC1)C(=O)N2
3-{1-[6-(6-fluoro-2,3-dihydro-indole-1-carbonyl)-pyrimidin-4-yl]-piperidin-4-yl}-7-methoxy-1,3,4,5-tetrahydro-benzo[d][1,3]diazepin-2-one

용매

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타Then the reaction mixture was purified by preparative HPLC-MS
  2. 2
    기타freeze-dried

실험 절차

100 mg (0.25 mmol) 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-pyrimidine-4-carboxylic acid and 35 mg (0.26 mmol) 6-fluoro-2,3-dihydro-1H-indole in 0.10 mL (0.71 mmol) TEA and 1.5 mL DMF were combined with 90 mg (0.28 mmol) TBTU and stirred for 1 h at RT. Then the reaction mixture was purified by preparative HPLC-MS. The product-containing fractions were combined and freeze-dried.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08829006B2uspto-grants-2014_09