- Versatile strategies for the solid phase synthesis of small heterocyclic scaffolds: [1,3,4]-Thiadiazoles and [1,3,4]-oxadiazoles
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New robust protocols for the solid phase synthesis of 5-alkylthio-, 5-alkyl/aryl-, and 5-acylamino-2-alkylamino-[1,3,4]-thiadiazoles are described based on a common resin bound thiosemicarbazide. A protocol for the solid phase synthesis of 2-alkyl/aryl-amino-5-alkylamino-[1,3,4]-oxadiazoles from a resin bound semicarbazide is likewise reported. The protocols have been verified by the preparation of four small libraries that all gave products in good to excellent yields and purity.
- Severinsen, Rune,Kilburn, John Paul,Lau, Jesper F.
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p. 5565 - 5575
(2007/10/03)
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- 1,3,4-THIADIAZOLES USEFUL FOR THE TREATMENT OF CMV INFECTIONS
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The present invention presents novel 1,3,4-thiadiazole derivatives of formula I which have useful antiviral activity against herpes virus, cytomegalovirus (CMV).
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- A new route to 1,2,4-triazoles and 1,3,4-thiadiazoles from 1-acylbithiourea
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The intramolecular cyclization of 1-acylbithiourea 1 gave 1,2,4-triazole 2 and 1,3,4-thiadiazole 3. The reaction of 1 with p-toluenesulfonyl chloride in the presence of triethylamine afforded 3. Treatment of 1 with methyl iodide in the absence of any base yielded 2-methylthio-1,3,4-thiadiazole 10 and 2-imino-1,3,4-thiadiazoline 12.
- Okawara,Tateyama,Yamasaki,Furukawa
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p. 1071 - 1075
(2007/10/02)
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