A convergent synthesis of an LTD4 antagonist, RG12525
β Scribed by Adam W. Sledeski; Michael K. O'Brien; Larry K. Truesdale
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- French
- Weight
- 206 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0040-4039
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β¦ Synopsis
An efficient, convergent synthesis of an LTD 4 antagonist, RG12525 (1) has been achieved through the alkylation of the (2-quinolinylmethoxy)phenol (2) with either a triphenylmethyl protected tetrazole synthon (4a) or with a tetrahydropyranyl derivative (4b). Preparation of synthons 4a and 4b, as well as novel preparation of 2 is described.
π SIMILAR VOLUMES
An efficient, 9-step synthesis of LTD4 antagonist L-708,738 is described. The asymmetric center is set via a chiral borane reduction.
## Abstract The synthesis of 5β[3β{2β(7βchloroquinolinβ2βyl)ethenyl}βphenyl]β8βdimethylcarbamylβ4,6β[6β^35^S]dithiaoctanoic acid at a specific activity of 1350 Ci/mmol is reported. This compound is a reagent suited for selective affinity binding studies at the LTD~4~ receptor.
The synthesis of (E)-5-(3-(2-(7-~hloroquinolin-2-yl)ethenyl)-phen~l)-[5-~~C]-4,6-dith~anonane dicarboxylic acid N.Ndimethylamide (I1 4C]MK-571), a high-allinity LTD4 antagonist , from sodium [ l 4C]cyanide via a five step sequence is described. Condensation of 3-[14C]cyanobenzaldehyde with 7-chloroq