Improved syntheses of N-Desmethylcitalopram and N,N-Didesmethylcitalopram
An improved and efficient synthesis of N-desmethylcitalopram (2) and N,N-didesmethylcitalopram (3) is presented. The method involved N-demethylation of citalopram (1) using 1-chloroethyl chloroformate to give 2 in 87% yield. Synthesis of 3 was accomplished by alkylation of 8 with 1-(3-bromopropyl)-2,2,5,5-tetramethyl-1-aza-2,5-disilacyclopentane (9).
Jin, C., Boldt, K., Rehder, K., & Brine, G. (2007). Improved syntheses of N-Desmethylcitalopram and N,N-Didesmethylcitalopram. Synthetic Communications, 37(6), 901-908. https://doi.org/10.1080/00397910601163745