Skin Diseases Interleukin-2 Inhibitors

Title Treatment of Skin Disorders Using Thieno[2,3-d]pyrimidinediones D. Cheshire et al., US Patent 6,984,644 (January 10, 2006) 

Invention Significance T-cells play an important role in the immune 

A method for inhibiting IL-2 transcription using thieno[2,3d]pyrimidine-2,4(lH,3H)-dione derivatives for the treatment of skin-related disorders is described. 

Palladium on carbon (10%, 1.00 g) was added to a suspension of 3-(l-naphthyl)acrylic acid (50.0 g) in 500 ml THF and hydrogenated 18 hours at 6 atm of hydrogen. The mixture was then filtered through a kieselguhr pad and the pad washed three times with 10 ml EtOAc. The filtrate was concentrated and 50.0 g product isolated as a solid. 

A solution of 7.40 ml oxalyl chloride dissolved in 50 ml CH2C12 was added dropwise to a suspension of the Step 1 product (8.50 g) in 100 ml CH2C12 containing 0.1ml DMF and stirred 2 hours at ambient temperature. The mixture was concentrated and the residual oil dried 4 hours in vacuo at 50°C. 

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