Fig. 2: Synthesis and structure of iP300w and stereoisomers. | Oncogenesis

Fig. 2: Synthesis and structure of iP300w and stereoisomers.

From: Inactivation of the CIC-DUX4 oncogene through P300/CBP inhibition, a therapeutic approach for CIC-DUX4 sarcoma

Fig. 2

A Structures of iP300w and A-485. B Synthesis pathway, reagents and conditions: a KCN, (NH4)2CO3, EtOH, H2O, 70 °C; b sodium 2-iodobenzenesulfonic acid, (CH3CH2CH2CH2)4N(HSO4), Oxone, MeCN, 65 °C; c bromoacetyl bromide, DCM, RT; d K2CO3, DMF, 5 °C, followed by preparative chromatography; e N-methyl-2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)acetamide, Pd(dppf)Cl2.CH2Cl2, K2CO3, 1,4-dioxane, H2O, 95 °C; f NaBH4, THF, MeOH, 0 °C; g DAST, DCM, −70 °C.

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