Christopher G. Newton

Large scale asymmetric synthesis of a biologically active sulfoxide

Abstract The asymmetric synthesis of sulfoxide RP 73163 is described. The synthetic strategy is based on the enantioselective oxidation of a suitably designed prochiral methyl sulfide, followed by α alkylation of the resulting sulfoxide.

Bis-deoxygenation of methyl 3,6-anhydro-D-pyranosides

Abstract The synthesis and radical reduction of thiocarbonyl derivatives of methyl 3,6-anhydro pyranosides has been studied in the α-D-gluco, α-D-manno and β-D-galacto series. A cyclic intermediate is proposed to explain the fact that bis-deoxygenation only occurred in the galactose series, providing a 3 step synthesis of the desired product 1b .

Patenting combinatorial libraries and associated technologies: a review of the last 12 months

Patents filed over the last 12 months are reviewed to see if patenting strategies are changing.

Editorial Biologicals & Immunologicals: Patenting combinatorial libraries and associated technologies

The advent of combinatorial chemistry in all its manifestations has the potential to change radically the patenting strategies of all pharmaceutical organisations. This editorial reviews recent progress over the past three years.

Cyclic meso-ionic heterocycles. Part 24. The reaction of 1,2-dithiolium-4-olates with aniline. The formationof 11-phenylbenz[b]indeno[2,1-e]-1,4-thiazine

Abstract Reaction of the type B meso-ionic heterocycle 3,5-diphenyl-1,2-dithiolium-4-olate (1) with aniline yields N-phenyl-(3-phenyl-1-phenylimino-inden-2-yl)-amine (10) and 11-phenylbenz[bindeno[2,1-e]-1,4-thiazine (12). Mechanistic investigations establish that the 3-phenylindenylamine (10) is an intermediate in the formation of the tetracyclic 1,4-thiazine (12).

Molecular Diversity in Drug Design. Application to High-speed Synthesis and High-Throughput Screening

The goal of High Speed Synthesis, High Throughput Screening and Molecular Diversity technologies in the pharmaceutical industry is to reduce the cost of finding good quality leads against a pharmaceutical target. Good quality leads should allow faster optimisation to candidate drugs. It is vital to maintain this perspective when discussing the advantages of these enabling technologies and the large costs associated with their implementation and running. The focus of this paper will be on reviewing the factors that seems to explain why some compounds are better leads and candidate drugs than others. This will help to set out the strategic decisions that have to be made, to try to optimise the benefits and synergies of HSS, HTS and diversity. The conclusion is that considerations of pharmacological conformity — that the molecules designed have the best chance of being fit-for-purpose — should be placed before considerations of how diverse molecules are from one another.

Patenting combinatorial libraries and associated technologies: a review of June 1997 to November 1998

Patent applications published June 1997 - November 1998 are reviewed to see how trends are evolving with time. Patents are divided into three subtypes: enabling chemistries, equipment and technologies, and therapeutic inventions using libraries. More than 170 patents reviewed testify to this explosive area. Nonetheless, many patents may require their claims amending before granting, and may also be very difficult to defend. Attention is drawn to articles from patent attorneys discussing the difficulties in prosecuting patents in this technology.