The Synthesis of Some 2-Substituted Morpholines

F. Loftus

Synthetic Communications · 1980 · 10.1080/00397918008080054

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★ 4.0 1 rating
5 : Major extension (new functional group)
4 : Minor extension (no new functional group) ×1
3 : Reproduced as published
2 : Reproduced with deviation
1 : Did not work
: Extension failed / Inconclusive

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PhD student
13 Jul 2026
★ 4 : Minor extension (no new functional group)

The synthesis of chloromethyl morpholine 1, worked well without purification. The reaction conditions are quite harsh, but the crude black tar after extraction resulted in a clean crude product by 1H-NMR.

The reaction was further extended for a 7 membered chloromethyl oxazepane and two methyl substituted systems. To read more details about how we ran the reactions and our attempts of extension, please read the supporting information of "Short Scalable Route to Bis-morpholine Spiroacetals and Oxazepane Analogues: Useful 3D-Scaffolds for Compound Library Assembly" and look up compounds 1, S32, 32, and 36.