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The present work describes the synthesis of sila-venlafaxine, disila-bexarotene, disila-AG-045572 (disila-CMPD1), a series of silicon-based allosteric modulators of muscarinic receptors, and a partial synthesis of sila-gabapentin. Crystal structure data of rac-sila-venlafaxine hydrochloride, (R)-sila-venlafaxine hydrobromide, bexarotene, disila-bexarotene, and disila-AG-045572 (disila-CMPD1) are included. Studies on the biological activities of sila-venlafaxine and of silicon-based allosteric modulators of muscarinic receptors are discussed. The Si-2,4,6-trimethoxyphenyl (Si-2,4,6-TMOP) moiety is described as a novel, acid-labile protecting group in organosilicon chemistry. The synthesis of chlorotris(chloromethyl)silane and tris(chloromethyl)methoxysilane is described.