Patent ID: 7015321

Claim:
A process for the synthesizing a mono-protected, non-symmetrical cyclic sulfamide III from an amino alcohol I and Burgess reagent II represented by the following structures: the process comprising the following steps: Step A: contacting a solution of the amino alcohol I in a non-reactive solvent with a quantity of the Burgess reagent II for producing sulfamide III; then, after consuming amino alcohol I Step B: neutralizing the reaction of said Step A by dilution with a non-reactive solvent and treatment with an aqueous solution; and then Step C: isolating sulfamide III; wherein: X is absent or is a diradical selected from the group consisting of the following structures: R 1 is a radical selected from the group consisting of hydrogen, C 1 –C 6 alkyl, aryl, heteroaryl, alkylaryl, and benzyl, or is a diradical forming a ring with R 2 ; R 2 is a radical selected from the group consisting of hydrogen, C 1 –C 6 alkyl, aryl, heteroaryl, alkylaryl, and benzyl, or is a diradical forming a ring with R 1 or R 3 or R 4 , or is a diradical forming a part of an aromatic ring with R 5 ; R 3 is a radical selected from the group consisting of hydrogen, C 1 –C 6 alkyl, aryl, heteroaryl, alkylaryl, and benzyl, or is a diradical forming a ring with R 1 or R 2 or R 5 or is a diradical forming half of a π-bond with R 6 ; R 4 is a radical selected from the group consisting of hydrogen, C 1 –C 6 alkyl, aryl, heteroaryl, and benzyl or is a diradical forming a ring with R 2 or with R 5 ; R 5 is a radical selected from the group consisting of hydrogen, C 1 –C 6 alkyl, aryl, heteroaryl, alkylaryl, and benzyl, or is a diradical forming a ring with R 1 or R 2 or R 6 or is a diradical forming part of an aromatic ring with R 3 ; R 6 is a radical selected from the group consisting of hydrogen, C 1 –C 6 alkyl, aryl, heteroaryl, alkylaryl, and benzyl, or is a diradical forming a ring with R 1 or R 2 or R 5 or is a diradical forming half of a π-bond as part of an aromatic ring with R 3 ; R 7 is a radical selected from the group consisting of hydrogen, C 1 –C 6 alkyl, aryl, heteroaryl, alkylaryl, and benzyl; Y is a radical selected from the group consisting of —CH 3 , —CH 2 Ph and —CH 2 CH═CH 2 ; with the following proviso: if R 2 and R 5 are part of an aromatic ring; then R 3 and R 6 make up a full π-bond; if X is absent, then R 3 cannot be half of a π-bond and R 2 is not part of an aromatic ring.