Unprecedented "In Water" imidazole carbonylation: paradigm shift for preparation of urea and carbamate |
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| Authors: | Padiya Kamlesh J Gavade Sandip Kardile Bhavana Tiwari Manojkumar Bajare Swapnil Mane Madhav Gaware Vivek Varghese Shaji Harel Dipak Kurhade Suresh |
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| Institution: | Department of Medicinal Chemistry, Nycomed Pharma Pvt. Ltd., 29-31 Suren Road, Andheri east, Mumbai-400 092, India. kamleshpadiya@lupinpharma.com |
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| Abstract: | The first "In Water" imidazolecarbonylation of amine is described. A one pot reaction of carbonylimidazolide in water with a nucleophile provides an efficient and general method for the preparation of urea, carbamates and thiocarbamates. Use of an anhydrous solvent and an inert atmosphere could be avoided. Product precipitate out from the reaction mixture and can be obtained in high purity by filtration, resulting in a simple and scalable method. |
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