Cui‐Feng Yang
2010
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Journal
Applied Chemical Industry
Abstract
Two ways in synthesis of pharmaceutical intermediate 1-(tert-butyl)-3-amioazetidine were investigated by 1-(tert-butyl)-3-hydroxyazetidine as raw materials,sodium azide and phthalimide potassium salt as the ammonia source,and experiments operability,security,yield and post-processing level of them were studied.Experiments showed that when using azide as the ammonia source to replace the hydroxyl into azido,then adding zinc powder can be reduced to the product,obtained 70% yield.However,sodium azide may be toxic,the operation is more difficult due to its explosion when heat or vibration.When potassium phthalimide was used as the ammonia source,the product was obtained by hydrazinolysis the tert-ammonia solution in hydrazine hydrate.The yield was 63%,though lower than the fomer method,but the experiment could be operational very strong,safe and simple post-processing.