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Temozolomide- Mr kiss kiss bang bang

It’s not often that drug molecules find themselves on the reagent shelf alongside materials that may have been used to assemble them. The prince and the pauper so to speak. In 2019 Paul Hergenrother from the University of Illinois published a paper in Angewandte Chemie claiming a diazomethane surrogate that was a commercially available, weighable, solid:

A couple of interesting papers from Angewandte Chemie

1. Using an approved drug as a diazomethane surrogate1 A recent paper published in Angewandte Chemie describes the use of Temozolomide (TMZ) as a solid weighable diazomethane surrogate. TMZ is an approved drug and is the standout treatment for gliobastoma.  It is stable weighable solid, with reasonable water solubility.  Under physiological conditions , pH 7.4,

Intrinsically safe and shelf stable diazo transfer reagent for fast synthesis of diazo compounds

At the Scientific Update OPRD conference in Milan earlier this month, Xiaohu Deng from Kura Oncology discussed a pyrimidine-derived diazo intermediate that exists predominantly in the tautomeric ‘tetrazole’ form at equilibrium in solution.[1] The compound was shown as a putative retrosynthetic building block for synthesis of a J&J P2X7 antagonist (Figure 1).[2] I’d not come

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