Reaktion #52955

Reaktionsgleichung

2,6-dimethoxy-4-(thiomorpholinomethyl)-benzeneboronic acid

N-(2,6-dichlorobenzoyl)-4-bromo-L-phenylalanine ethyl ester

K2CO3

→

N-(2,6-dichlorobenzoyl)-4-[2,6-dimethoxy-4-(thiomorpholinomethyl)phenyl]-L-phenylalanine ethyl ester

Ausbeute 15.2%

Lösungsmittel

DME H2O

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigepurified

Vorschrift

A mixture of 2,6-dimethoxy-4-(thiomorpholinomethyl)-benzeneboronic acid (1.1 g), N-(2,6-dichlorobenzoyl)-4-bromo-L-phenylalanine ethyl ester (0.71 g), Pd(PPh3)4 (1.0 g) and K2CO3 (1.00 g) in DME/H2O (10 mL/0.5 mL) was heated at 80° C. for 6 h under N2. The mixture was worked up and purified according to the procedure described in Example 8-3) to yield 0.15 g of N-(2,6-dichlorobenzoyl)-4-[2,6-dimethoxy-4-(thiomorpholinomethyl)phenyl]-L-phenylalanine ethyl ester. mp. 86-89° C. ESMS: m/z 616 (MH+). HCl salt: mp. 204-205° C.

Quelle