(conversion of pyrimidine-2-carbonitrile derivative to pyrimidine-2-carboximidamide)
Dear Mohammed,
You may react pyrimidine-2-carbonitrile derivative with dry ammonia in acetic acid to furnish the corresponding pyrimidine-2-carboximidamide derivative. For more on this reaction, please see Scheme 1 in the attached publication.
Hoping this will be helpful,
Rafik
Using H2SO4 (70%) and heating at 60- 700C for about 6-8 hr, then pouring onto water, filter the product (carboximide), dry it well and pass stream of dry ammonia gas in an methanolic solution of the carboximide for enough time (about 2hr).
thanks, dear prof
but my problem now is the ammonia gas
its not available :)
links for preparation of ammonia gas:
https://youtu.be/4epBHiBbbmU
https://youtu.be/I_DD2_7QkRk
https://youtu.be/gh4gGkk74iU
Aromatic nitrile to amidine.
Nitrile to thioamide by bubling dry H2S in a Pyridine-Triethylamine mixture.
Thioamide to amidine by methyl iodide folowed by treatment with amonium acetate.
See also Pinner reaction.
Passing HCl gas for few hrs followed by passing dry ammonia gas for another few hrs.
Ammonia can be generated using NH4Cl sat solution + NaOH solid and passing the gas over NaOH trap to dry it.
Use Ammonium chloride+HCl or use SSA and Ammonium hydroxide at room temprature
Dear all
the most appropriate method is to dissolve the start in THF and add 10mL of 1M (Lithium bis(trimethylsilyl)amide) dropwise over 1h then left at rt for 8h, after that, 5mL of saturated ethanolic HCl was added while the mixture was in ice bath, the reaction completion was monitored by TLC
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