Isis Pharmaceuticals, Inc.

Other

Robert H Springer

Phillip Dan Cook

Bruce S Ross

Kelly G Sprankle

Yogesh S Sanghvi

Rich H Griffey

Oscar L Acevedo

Robert S Andrews

Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2&prime; and 5&prime; positions. Monomeric sub-units having these modifications may be further modified at the 2&prime; position. Improved processes for the synthesis of 2&prime;-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2&prime;-anhydropyrimidine nucleoside or a 2S,2&prime;-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

Process for the synthesis of 2&prime;-O-substituted pyrimidines and oligomeric compounds therefrom

Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2&prime; and 5 positions. Monomeric sub-units having these modifications may be further modified at the 2 position. Improved processes for the synthesis of 2&prime;-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2&prime;-anhydropyrimidine nucleoside or a 2S,2&prime;-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

Improved processes for the synthesis of 2'-O-substituted pyrimidine nucleosides are provided. The processes feature alkylation of a 2,2'-anhydropyrimidine nucleoside or a 2S,2'-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

Process for the synthesis of 2'-O-substituted pyrimidines

For large scale preparation of pyrimidine ribonucleosides, the intermediate 2-O-methyl-(or ethyl)-1,3,5-tri-O-benzoyl-.alpha.-D-ribose can be prepared using a diazomethane (or diazoethane) reaction that is controlled via an inert solvent transferring system. This transfer system allows for large scale preparations of the pyrimidine ribonucleosides.

Apparatus and processes for the large scale generation and transfer of

A multi-purpose hexagonal building module constructed of identically configured panels connected together at lap joints, with each panel having a large flat rectangular section and an integral smoothly curved section. When the panels are interconnected to form a hexagonal module, the relatively large rectangular flat sections collectively constitute the module's six planar walls and the relatively small smoothly curved panel sections function as rounded module corners. The module can be disposed with its central symmetrical axis vertical or horizontal, and can be used as a housing unit or as a container for product storage. The module, whether used for storage or as a living unit, and whether disposed horizontally or vertically, can be permanently mounted at a single site or made mobile by mounting on a vehicle or ship for transport across land or water. The module is relatively inexpensive in terms of cost of material and assembly, exhibits substantial structural strength against loads of various types in an axial, horizontal, or torsional direction, and is readily erected with simple tools and without special skills. The modules can be stacked vertically to form a multi-level building, arranged compactly in a tightly nested honeycomb arrangement, or spaced horizontally and interconnected by filler panels for a more expansive building.

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Carlsbad, CA, United States of America

Robert H Springer