- Synthesis method of 2-([1, 1 '-biphenyl]-4-yl)-2-glycine compound
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The invention relates to a synthesis method of a 2-([1, 1 '-biphenyl]-4-yl)-2-glycine compound. The method comprises the following steps: performing suzuki reaction on a compound as shown in a formulaI and a compound as shown in a formula II in the presence of alkali, a solvent and a catalyst under inert gas protection and microwave-assisted conditions to prepare an intermediate compound, and then deprotecting the intermediate compound to prepare a compound as shown in a formula III, wherein the structural formula of the compound shown in the formula I is shown in the specification, the structural formula of the compound shown in the formula II is shown in the specification, the structural formula of the compound shown in the formula III is shown in the specification, and in the formula Iand the formula III, R is one of H, alkyl, alkoxy, halogen and trifluoromethyl. The synthesis method is low in toxicity, high in safety coefficient, easy and convenient to operate, easy to control and efficient in reaction, and the yield reaches up to 81% or above. In the synthesis method, microwave assistance is added for a certain time in the suzuki reaction process, so that the reaction is promoted, the reaction efficiency is effectively improved, and the reaction time is shortened.
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Paragraph 0061-0067; 0173-0184
(2020/11/10)
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- Synthesis of Unprotected 2-Arylglycines by Transamination of Arylglyoxylic Acids with 2-(2-Chlorophenyl)glycine
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The transamination of α-keto acids with 2-phenylglycine is an effective methodology for directly synthesizing unprotected α-amino acids. However, the synthesis of 2-arylglycines by transamination is problematic because the corresponding products, 2-arylglycines, transaminate the starting arylglyoxylic acids. Herein, we demonstrate the use of commercially available l-2-(2-chlorophenyl)glycine as the nitrogen source in the transamination of arylglyoxylic acids, producing the corresponding 2-arylglycines without interference from the undesired self-transamination process.
- Inada, Haruki,Shibuya, Masatoshi,Yamamoto, Yoshihiko
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p. 11047 - 11059
(2020/10/12)
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