Simple and efficient synthesis of racemic 2-(tert-butoxycarbon-ylamino)-2-methyl-3-(1H-1,2,4-triazol-1-yl)propanoic acid, a new derivative of β-(1,2,4-triazol-1-yl)alanine.

A simple synthetic approach to racemic N-tert-butyloxycarbonyl-2-methyl-3-(1H-1,2,4-triazol-1-yl)alanine (5) in four steps and 68% overall yield starting from oxazoline derivative 1 is reported. This synthesis involves the alkylation of 1H-1,2,4-triazole with an O-tosyloxazoline derivative, followed by an oxazoline ring-opening reaction and oxidation of the N-protected β‑aminoalcohol by potassium permanganate.

10-(Prop-2-yn-yl)-10H-phenothia-zine.

In the mol-ecule of the title compound, C(15)H(11)NS, the butterfly angle between the two planes defined by the two wings of the phenothia-zine unit is 33.5 (8)°. The dihedral angles between the two benzene rings and the propynyl group are 85 (4) and 63 (4)°.

2-(1,3-Dioxoisoindolin-2-yl)acetonitrile.

The asymmetric unit of the title compound, C(10)H(6)N(2)O(2), contains two independent mol-ecules. The dihedral angles between the acetonitrile and the 1H-isoindole-1,3(2H)-dione units are 69.0 (7)° and 77.

N-(Cyano-meth-yl)benzamide.

In the structure of the title compound, C(9)H(8)N(2)O, the amide group is twisted by a dihedral angle of 21.86 (7)° with respect to the benzene ring, while the planes of the benzene ring and cyano-methyl group form a dihedral angle of 53.13 (11)°.

Synthesis of new alpha-heterocyclic alpha-aminoesters.

alpha-Heterocyclic alpha-aminoesters were obtained in good yields by reaction of a glycine cation equivalent and different heterocyclic nucleophiles; diastereoselectivity using a carbohydrate (galactopyranose) as N-protecting group was modest.