90005-62-2Relevant academic research and scientific papers
Scalable, Telescoped Hydrogenolysis-Enzymatic Decarboxylation Process for the Asymmetric Synthesis of (R)-α-Heteroaryl Propionic Acids
Blakemore, Caroline A.,France, Scott P.,Samp, Lacey,Nason, Deane M.,Yang, Eddie,Howard, Roger M.,Coffman, Karen J.,Yang, Qingyi,Smith, Aaron C.,Evrard, Edelweiss,Li, Wei,Dai, Linlin,Yang, Lixia,Chen, Zhiguang,Zhang, Qingli,He, Fangyan,Zhang, Jiesen
supporting information, p. 421 - 426 (2020/11/12)
Enantiopure α-aryl propionic acids are useful building blocks for pharmaceutical research and can be accessed enzymatically using arylmalonate decarboxylases (AMDases) from the corresponding malonic acids. However, the intrinsic instability of malonic acids is a major drawback to this approach in which spontaneous decarboxylation can occur, subsequently eroding enantioselectivity and giving rise to racemic products. This was particularly evident for a panel of N-heterocyclic propionic acids that we wished to access using the approach. Herein, we describe a process to overcome the spontaneous decarboxylation problem in which hydrogenolysis of the corresponding dibenzyl malonates was performed in a biphasic toluene-basic aqueous buffer mixture and telescoped into the subsequent AMDase step. This procedure enabled compounds to be accessed in high enantioselectivities and was successfully demonstrated on 120 g with high yield (76%) and ee (98%).
Pyridineacetamide derivative serving as CDK inhibitor, and preparation method and application thereof
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Paragraph 0383; 0386; 0389-0390, (2021/07/28)
The invention belongs to the technical field of pyridineacetamide derivatives, and particularly relates to a pyridineacetamide derivative serving as a CDK inhibitor and a preparation method and application of the pyridine acetamide derivative. The pyridineacetamide derivative shows excellent CDK9/CDK7 enzyme inhibitory activity, and can be used for preparing drugs used for treating cancers, especially hematologic cancers including acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, follicular lymphoma and the like and solid tumors such as breast cancer, prostate cancer, ovarian cancer, hepatocellular carcinoma, pancreatic cancer, kidney cancer, stomach cancer, colorectal cancer, lung cancer and the like.
Preparation method of organic carboxylic acid
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Paragraph 0062-0064, (2019/10/15)
The invention discloses a preparation method of organic carboxylic acid. The preparation method comprises the following steps that catalysts, olefins, water and solvents are added into a reaction container; CO is introduced; heating reaction is performed; after the reaction completion, separation is performed to obtain organic carboxylic acid; the catalysts comprise transition metal catalysts, ligands and catalysis assistants; the catalysis assistants comprise Lewis acid salt. The preparation method has the advantages that the dependency on protonic acid in the prior art is avoided; the Lewisacid salt is used as the catalysis assistant, so that the corrosion of a reaction system on equipment can be effectively prevented; the requirements on equipment are lowered. The preparation method has excellent substrate practicability; the operation steps are simple and fast; the reaction conditions are mild and are easy to control; the raw materials are cheap and can be easily obtained; the product yield and the product purity are high; the preparation method is suitable for large-scale industrial production; the normal/iso ratio of reaction products can be regulated and controlled throughthe catalysis assistants; the defects of regulating and controlling the normal/iso ratio of the reaction products by traditional phosphine ligands are overcome; the reaction progress of the reaction is simplified; the cost is favorably reduced.
Regioselectivity inversion tuned by iron(iii) salts in palladium-catalyzed carbonylations
Huang, Zijun,Cheng, Yazhe,Chen, Xipeng,Wang, Hui-Fang,Du, Chen-Xia,Li, Yuehui
supporting information, p. 3967 - 3970 (2018/04/23)
Impactful regioselectivity control is crucial for cost-effective chemical synthesis. By using cheap and abundant iron(iii) salts, the hydroxycarbonylations of both aromatic and aliphatic alkenes were significantly enhanced in both reactivity and selectivity (iso/n or n/iso up to >99:1). Moreover, Pd-catalyzed carbonylation selectivity can be switched from branched to linear by using different Fe(iii) salts. In addition, similar results were obtained for the carbonylation of secondary alcohols.
