1212-53-9Relevant articles and documents
A highly efficient flow reactor process for the synthesis of N-Boc-3,4-dehydro-l-proline methyl ester
Tamborini, Lucia,Conti, Paola,Pinto, Andrea,Micheli, Carlo De
, p. 222 - 225 (2010)
The multi-step preparation of N-Boc-3,4-dehydro-l-proline methyl ester using a modular flow reactor is reported. The use of immobilised reagents and scavengers in pre-packed glass tubes allows us to obtain the pure product in 87% overall yield, 97% purity, and >98% enantiomeric excess without any additional purification step. Our flow-based protocol enables the rapid multi-gram synthesis (about 9 g/12 h) of the desired product.
Preparation method of carboxylic ester compound
-
Paragraph 0042-0043, (2021/03/30)
The invention relates to a preparation method of a carboxylic ester compound, which comprises the following steps: reacting carboxylic acid with methanol in air under the catalysis of nitrite to obtain an ester compound, the preparation method disclosed by the invention has the advantages of rich raw material sources, cheap and easily available catalyst, mild reaction conditions, simplicity and convenience in operation and the like, a series of fatty carboxylic acids can be modified with high yield, and particularly, the traditional esterification method is generally not suitable for esterification of drug molecules. By utilizing the method, a series of known drug molecules can be modified, so that a shortcut is provided for discovering new drug molecules.
Electrochemical Dimethyl Sulfide-Mediated Esterification of Amino Acids
Li, Yongli,Wang, Huamin,Zhang, Heng,Lei, Aiwen
supporting information, p. 3023 - 3028 (2021/08/30)
Dimethyl sulfide-mediated electrochemical synthetic strategy for esterification of amino acids has been reported. A series of amino acids could react smoothly with alcohols, affording the desired esterification products with good efficiency. Importantly, the tolerance of peptides and gram-scale synthesis shed light on the utility of this protocol. Mechanistically, the dimethyl sulfide as a mediator plays an essential role in the transformation of amino acids.
An efficient, stereocontrolled and versatile synthetic route to bicyclic partially saturated privileged scaffolds
Bond, Andrew D.,Hanby, Abigail R.,King, Thomas A.,Moss, Thomas A.,Sore, Hannah F.,Spring, David R.,Stewart, Hannah L.
supporting information, p. 6818 - 6821 (2020/07/04)
Herein, we describe the development of a simple, high yielding and stereocontrolled strategy for the synthesis of a series of triazolopiperazines and other biologically relevant fused scaffolds from optically active amino acids. This route was applied to the synthesis of 22 scaffolds containing new, previously inaccessible vectors and used to access a novel analogue of ganaplacide.
