2978-58-7Relevant articles and documents
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Engel,P.S.,Bishop,D.J.
, p. 6754 - 6762 (1975)
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Preparation method for propyzamide
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, (2018/05/01)
The invention discloses a preparation method for propyzamide. The preparation method comprises the following steps: preparing 3-chloro-3-methylbutyne through a chlorination reaction; then preparing 3-amino-3-methylbutyne through an aminolysis reaction; and then carrying out an amidation reaction so as to prepare high-purity propyzamide. The optimal preparation method for propyzamide is screened out through a large number of experiments; the preparation method is reasonable in the whole process design and simple and efficient in process operation; in particular, optimal reaction conditions arescreened out, optimal raw material composition is determined for the chlorination reaction in the step 1, the aminolysis reaction in the step 2 and the amidation reaction in the step 3, and the proportions of reaction raw materials, reaction temperature, reaction time and the like are optimized, so reaction yield can be greatly increased (wherein the yield can reach 93% or more), side reactions can be reduced, reaction rate can be increased, and production cost can be greatly lowered; so the preparation method has good application prospects.
Cu(I)-catalyzed synthesis of dihydropyrimidin-4-ones toward the preparation of β- And β3-amino acid analogues
Rajagopal, Basker,Chen, Ying-Yu,Chen, Chun-Chi,Liu, Xuan-Yu,Wang, Huei-Ren,Lin, Po-Chiao
supporting information, p. 1254 - 1264 (2014/03/21)
A copper(I)-catalyzed synthesis of substituted dihydropyrimidin-4-ones from propargyl amides via the formation of ketenimine intermediate has been successfully developed; the synthesis afforded good isolated yields (80-95%). The mild reaction conditions at room temperature allow the reaction to proceed to completion in a few hours without altering the stereochemistry. Further, by involving a variety of reactive nucleophiles, the obtained substituted dihydropyrimidin-4-ones were elegantly transformed into the corresponding β- and β3-amino acid analogues.
Preparation of a Series of Highly Hindered Secondary Amines, Including Bis(triethylcarbinyl)amine
Kopka, Ihor E.,Fataftah, Zacharia A.,Rathke, Michael W.
, p. 4616 - 4622 (2007/10/02)
A series of highly branched secondary amines was prepared by coupling propargylamines with propargyl chlorides.Hydrogenation of the resultant dipropargylamines was accomplished with Raney nickel in the presence of potassium hydroxide.The resultant amines, including bis(triethylcarbinyl)amine, are among the most hindered secondary amines reported to date.The pKa values of the conjugate acids of the series of secondary amines exhibit a regular decrease with increasing size of the amine.The bulkier members of the series are inert to methyl iodide.Bis(triethylcarbinyl)amine reacts with boron trifluoride etherate to give a primary amine adduct and 3-ethyl-2-pentene.