Reaction #456383

ord-04f9233ca35a4d5a8bdd161add6d8a95

Reaction equation

O=C([O-])O.[Na+]
sodium bicarbonate
O=C(N[C@@H](Cc1ccc(-c2cccs2)cc1)C(=O)O)C(CS)Cc1ccccc1
N-[(1,1-dimethylethoxy) carbonyl]-O-[(trifluoromethyl) sulphonyl]-L-tyrosine
O=C(N[C@@H](Cc1ccc(-c2cccs2)cc1)C(=O)O)C(CS)Cc1ccccc1
(S)N-(2-(mercaptomethyl)-1-oxo-3-phenylpropyl]4- (2-thienyl)L-phenylalanine
OB(O)c1cccc2ccccc12
naphthalene boronic acid
O=C(N[C@@H](Cc1ccc(-c2cccc3ccccc23)cc1)C(=O)O)C(CS)Cc1ccccc1
expected product
O=C(N[C@@H](Cc1ccc(-c2cccc3ccccc23)cc1)C(=O)O)C(CS)Cc1ccccc1
(S)N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]4-(1-naphthyl)-L-phenylalanin

Solvents

Conditions

Detailed conditions
See reaction.notes.procedure_details.

Procedure

The operation is carried out as in Stage 1 of Example 10 starting with methyl ester of N-[(1,1-dimethylethoxy) carbonyl]-O-[(trifluoromethyl) sulphonyl]-L-tyrosine (prepared as indicated in Stage 1 of Example 10), 10 ml of toluene, 282 mg of naphthalene boronic acid and 169.7 mg of sodium bicarbonate, the solution is agitated for 15 minutes, then 94.77 mg of 5-tetrakis (triphenylphosphine) is added. In this way 165.7 mg of expected product is obtained.

Source

DOI: 10.6084/m9.figshare.5104873.v1Patent: US06136842uspto-grants-2000_10