17012-21-4Relevant articles and documents
Aminoborohydrides. 11. Facile reduction of N-alkyl lactams to the corresponding amines using lithium aminoborohydrides
Flaniken, John M.,Collins, Christopher J.,Lanz, Marc,Singaram, Bakthan
, p. 799 - 801 (1999)
Formula presented Various five- and six-membered N-alkyl lactams were reduced to the corresponding cyclic amines using lithium N,N-dialkylaminoborohydrides (LAB). Most of the reductions were essentially complete after refluxing in THF for 2 h. The cyclic amine products were easily isolated after an aqueous workup in very good to excellent yields. It is possible to selectively reduce most functional groups, such as esters, in the presence of a lactam using LAB reagents.
Discovery of the PARP (poly ADP-ribose polymerase) inhibitor 2-(1-(4,4-difluorocyclohexyl)piperidin-4-yl)-1H-benzo[d]imidazole-4-carboxamide for the treatment of cancer
Chen, Dawei,Jiang, Yuyang,Shi, Zhichao,Tang, Lin,Wu, Weibin,Zhai, Xin,Zhang, Cunlong
supporting information, (2021/07/28)
In this work, two series of cyclic amine-containing benzimidazole carboxamide derivatives were designed and synthesized as potent anticancer agents. PARP1/2 inhibitory activity assays indicated that most of the compounds showed significant activity. The in vitro antiproliferative activity of these compounds was investigated against four human cancer cell lines (MDA-MB-436, MDA-MB-231, MCF-7 and CAPAN-1), and several compounds exhibited strong cytotoxicity to tumor cells. Among them, 2-(1-(4,4-difluorocyclohexyl)piperidin-4-yl)-1H-benzo[d]imidazole-4-carboxamide (17d) was found to be effective PARP1/2 inhibitors (IC50 = 4.30 and 1.58 nM, respectively). In addition, 17d possessed obvious selective antineoplastic activity and noteworthy microsomal metabolic stability. What's more, further studies revealed that 17d was endowed with an excellent ADME profile. These combined results indicated that 17d could be a promising candidate for the treatment of cancer.
With antifungal activity of the wicked zuozuo apperception compound and its preparation method and application (by machine translation)
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Paragraph 0036-0038, (2017/09/02)
The invention discloses an oxazole compound with anti-fungal activity, a preparation method of the oxazole compound and an application of the oxazole compound to tobacco powdery mildew original fungi or cotton anthracnose original fungi prevention, and belongs to the technical field of organic synthesis. The technical scheme mainly includes that the oxazole compound with the anti-fungal activity is provided with a structure shown in the instruction, R1 refers to propiono, isopropyl, acetyl, ethyl or methyl, and R2 refers to dimethylamino or methylamine. Five oxazole compounds with the anti-fungal activity are synthesized by the novel method, the preparation process is simple in technology and easy to control, target product yield is high, repeatability is fine, and the five prepared oxazole compounds with the anti-fungal activity have a certain prevention function for tobacco powdery mildew original fungi or cotton anthracnose original fungi.
Synthesis of Orthogonally Protected 2,6-Diazaspiro[35]nonane and 2,6-Diazaspiro[3.4]octane Analogues as Versatile Building Blocks in Medicinal Chemistry
Orain, David,Hintermann, Samuel,Pudelko, Maciej,Carballa, Diego,Jedrzejczak, Anna
supporting information, p. 1815 - 1818 (2015/08/06)
A novel and efficient synthesis of orthogonally protected spirocyclic amines is described for the first time.
