Modular and divergent synthesis of 2,3-disubstituted 4-quinazolinones facilitated by regioselective -alkylation.

The synthesis of a biologically relevant 2-amino-3-alkylamido 4-quinazolinone has been accomplished in four steps from commercially available materials using design principles from both modular and divergent synthesis. 3-Alkylation of 2-chloro-4(3)-quinazolinone using methyl bromoacetate, followed by C2-amination produced a suitable scaffold for introducing molecular diversity. Optimization of alkylation conditions afforded full regioselectivity, enabling exclusive access to the -alkylated isomer.

The Evaluation and Treatment of Merkel Cell Carcinoma and Brain Metastasis: A Case Report and Review of the Literature.

Merkel cell carcinoma (MCC) is a rare and aggressive neuroendocrine tumor associated with high mortality if metastases are identified. Currently, there is no standardized nor curative treatment for neurometastatic MCC. In this study, we have reviewed the more recent cases and the use of immunotherapy in a population.