反応 #712142

ord-eb83b53140354078b9eebafe40de03b0

反応方程式

O=C(O)c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1
6-cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridine-2-carboxylic acid
C1COC2(C1)CNC2.Cl
5-oxa-2-azaspiro[3.4]octane hydrochloride
CN(C)C(On1nnc2ccccc21)=[N+](C)C.F[B-](F)(F)F
TBTU
CCN(C(C)C)C(C)C
DIEA
→
O=C(c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1)N1CC2(CCCO2)C1
title compound
O=C(c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1)N1CC2(CCCO2)C1
[6-Cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridin-2-yl]-(5-oxa-2-aza-spiro[3.4]oct-2-yl)-methanone

反応物

O=C(O)c1ccc(N2CC(F)(F)C2)c(OCC2CC2)n1
6-cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridine-2-carboxylic acid
C1COC2(C1)CNC2.Cl
5-oxa-2-azaspiro[3.4]octane hydrochloride
CN(C)C(On1nnc2ccccc21)=[N+](C)C.F[B-](F)(F)F
TBTU
CCN(C(C)C)C(C)C
DIEA

試薬

なし

反応条件

詳細条件
See reaction.notes.procedure_details.

実験手順

In analogy to the procedure described in Example 47 b), 6-cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridine-2-carboxylic acid (Example 1 b)) was reacted with 5-oxa-2-azaspiro[3.4]octane hydrochloride (1359656-11-3) in the presence of TBTU and DIEA to obtain the title compound as colorless oil; MS (EI): m/e=380.5 [MH+].

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US09303012B2uspto-grants-2016_04