Bristol-myers Squibb Compnay

The Scripps Research Institute

A Erik Rubin

K Barry Sharpless

Victor W Rosso

Harold Norris Weller, Iii

Joseph Nolfo

Alexander Bertok

Walter Ruediger

The base of the modular reactor includes a frame which defines an opening into which one of a plurality of interchangeable reaction vessel carrying inserts can be removeably received. Each insert has an array of recesses adapted to receive a different number of reaction vessels of different sizes. The recesses are positioned such that all arrays are suitable for use with a standard automated liquid handier. The frame has fluid flow channels for regulating the temperature of the lower portions of the vessels. A temperature control module can be received over the base to regulate the temperature of the upper portions of the vessels for reflux reactions. The corner radii of the insert and frame opening cooperate to permit the insert to be received in the frame in only one orientation. The walls of the insert are inclined to facilitate removal by a friction fit tool. Each vessel receiving recess has a self-centering conical or semi-circular shaped bottom to maximize heat transfer and distribute the load uniformly. The vessels seat as close to the bottom surface of the base as possible to facilitate use with an air driven magnetic stirrer. A thin, electrically heated plate may be received between the base and the stirrer.

Parallel chemistry reactor with interchangeable vessel carrying inserts

&agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.

Synthesis of &agr;,&bgr;-substituted amino amides, esters, and acids

Growing community of inventors

Plainsboro, NJ, United States of America

A Erik Rubin