反応 #2304281

ord-6ac5e631c7ad4b79bb21642bcc6237f1

反応方程式

Cl.NCC(=O)OCc1ccccc1
glycine benzylester hydrochloride
O=C(Cl)CCl
Chloroacetylchloride
Cl.NCC(=O)OCc1ccccc1
glycine benzylester hydrochloride
O=C([O-])[O-].[K+].[K+]
K2CO3
O=C(CCl)NCC(=O)OCc1ccccc1
N-(chloroacetyl)-glycine benzyl ester

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他was synthesized

実験手順

DOTA-G-tri-t-butyl ester 4, an intermediate compound in the synthesis of the conjugate 22, was synthesized starting with glycine benzylester hydrochloride (Aldrich), as described in Scheme 1. Chloroacetylchloride (Aldrich) was added to glycine benzylester hydrochloride in the presence of K2CO3 to produce N-(chloroacetyl)-glycine benzyl ester 1. The ester 1 was added to a suspension of DO3A-tri-t-butyl ester hydrochloride 2 (see U.S. Pat. No. 5,573,752) in K2CO3 to produce DOTA-G-tri-t-butyl-benzyl ester 3. Subsequent catalytic hydrogenation produced the DOTA-G-tri-t-butyl ester 4.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07407644B2uspto-grants-2008_08