15676-99-0Relevant academic research and scientific papers
Effect of additives on the stereochemical integrity and reactivity of α-alkoxycarbonyl alkenylcopper intermediates. Optimal conditions for the synthesis of isomerically pure tetrasubstituted alkenes
Zhu, Na,Hall, Dennis G.
, p. 6066 - 6069 (2003)
A systematic study on the effect of additives on the isomerizability of 1-alkoxycarbonyl alkenylcopper(I) intermediates revealed that the lithium chelator 12-crown-4 is significantly more efficient than HMPA at retarding isomerization. On the other hand, 12-crown-4 alone is unable to promote effective coupling with alkyl halides. The combination of 12-crown-4 and a reduced amount of HMPA, however, led to an improved procedure for the preparation of useful, isomerically pure tetrasubstituted alkenes such as allylation reagents and skipped dienes.
3 - Methyl pentyl acetate and flavoring agent -3 - mercapto
-
Paragraph 0061-0063, (2021/04/16)
To provide a novel flavoring agent.SOLUTION: Provided are a flavor improvement method of a perfume of a perfume composition comprising: a step of providing a flavoring agent comprising 3-mercapto-3-methyl pentyl acetate represented by the following formula (1), a flavoring agent containing it as an active ingredient, and a consumer goods containing the flavoring agent or the perfume composition; and, furthermore a step of blending the flavoring agent made of 3-mercapto-3-methyl pentyl acetate represented by the following formula (1) to the perfume composition, and a method of improving the perfume of the consumer goods comprising blending the flavoring agent or the perfume composition to the consumer goods.SELECTED DRAWING: None
SULFUR-CONTAINING COMPOUND AND FLAVORING AGENT
-
Paragraph 0085-0086, (2021/09/27)
PROBLEM TO BE SOLVED: To provide a novel sulfur-containing compound and a flavoring agent, a perfume composition and consumer goods, a method for improving flavor of the perfume composition, and a method for improving flavor of the consumer goods.SOLUTION: This invention provides: a sulfur-containing compound expressed by Formula (1); a flavoring agent comprising the compound expressed by Formula (1); a perfume composition containing the sulfur-containing compound or the flavoring agent; consumer goods containing the sulfur-containing compound, the flavoring agent or the perfume composition; a method for improving flavor of the perfume composition including a step of mixing the sulfur-containing compound or the flavoring agent into the perfume composition; and a method for improving flavor of the consumer goods including a step of mixing the sulfur-containing compound, the flavoring agent or the perfume composition into the consumer goods.SELECTED DRAWING: NoneCOPYRIGHT: (C)2021,JPOandINPIT
DIHYDROOROTATE DEHYDROGENASE INHIBITORS
-
Page/Page column 153-154, (2020/08/22)
Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Embodiments of such compounds are represented by Formula (I) as follows: 5 wherein R1, R2, R3, R4, R5a, R5b, X and Y, are defined herein.
DIHYDROOROTATE DEHYDROGENASE INHIBITORS
-
Page/Page column 75; 84, (2020/10/28)
Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, X, and Y are defined herein.
Novel diphenylmethyl compounds having mycobacterium tuberculosis inhibitory activity
-
Paragraph 0485-0488, (2019/02/13)
The invention relates to novel diphenylmethyl derivatives having mycobacterium tuberculosis inhibitory activity and a preparation method thereof and particularly relates novel diphenylmethyl derivatives having activity for inhibiting replicative and non-replicating mycobacterium tuberculosis and a preparation method thereof. In particular, the invention relates to compounds shown in the formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein the variables are as described in the specification. The invention also relates to the preparation method of the compounds and their pharmaceutical compositions and a use of the compounds in preparation of drugs for treating mycobacterium tuberculosis infection-caused diseases.
Derivatives of Natural Product Agrimophol as Disruptors of Intrabacterial pH Homeostasis in Mycobacterium tuberculosis
Wu, Jie,Mu, Ran,Sun, Mingna,Zhao, Nan,Pan, Miaomiao,Li, Hongshuang,Dong, Yi,Sun, Zhaogang,Bai, Jie,Hu, Minwan,Nathan, Carl F.,Javid, Babak,Liu, Gang
, p. 1087 - 1104 (2019/05/22)
This article reports the rational medicinal chemistry of a natural product, agrimophol (1), as a new disruptor of intrabacterial pH (pHIB) homeostasis in Mycobacterium tuberculosis (Mtb). Through the systematic investigation of the structure-activity relationship of 1, scaffold-hopping of the diphenylmethane scaffold, pharmacophore displacement strategies, and studies of the structure-metabolism relationship, a new derivative 5a was achieved. Compound 5a showed 100-fold increased potency in the ability to reduce pHIB to pH 6.0 and similarly improved mycobactericidal activity compared with 1 against both Mycobacterium bovis-BCG and Mtb. Compound 5a possessed improved metabolic stability in human liver microsomes and hepatocytes, lower cytotoxicity, higher selectivity index, and similar pKa value to natural 1. This study introduces a novel scaffold to an old drug, resulting in improved mycobactericidal activity through decreasing pHIB, and may contribute to the critical search for new agents to overcome drug resistance and persistence in the treatment of tuberculosis.
USE OF SUBSTITUTE OXO TETRAHYDROQUINOLINE SULFONAMIDES OR SALTS THEREOF FOR RAISING STRESS TOLERANCE OF PLANTS
-
Paragraph 0197, (2017/02/28)
The invention relates to the use of substituted oxotetrahydroquinolinylsulfonamides or salts thereof where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, and/or for increasing plant yield.
METABOTROPIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS OF USE THEREOF
-
Page/Page column 90, (2013/02/27)
Compounds that modulate GluR5 activity and methods of using the same are disclosed.
Catalytic asymmetric formation of δ-Lactones from Unsaturated acyl halides
Tiseni, Paolo S.,Peters, Rene
supporting information; experimental part, p. 2503 - 2517 (2010/09/03)
Previously unexplored enantiopure zwitterionic ammonium dienolates have been utilized in this work as reactive intermediates that act as diene components in hetero-Diels-Alder reactions (HDAs) with aldehydes to produce optically active δ-lactones, subunits of numerous bioactive products. The dienolates were generated in situ from E/Z mixtures of a,b- unsaturated acid chlorides by use of a nucleophilic quinidine derivative and Sn (OTf)2 as co-catalyst. The latter component was not directly involved in the cycloaddition step with aldehydes and simply facilitated the formation of the reactive dienolate species. The scope of the cycloaddition was considerably improved by use of a complex formed from Er- (OTf)3 and a simple commercially available norephedrine-derived ligand that tolerated a broad range of aromatic and heteroaromatic aldehydes for a cooperative bifunctional Lewis-acid-/ Lewis-base-catalyzed reaction, providing a,b-unsaturated d-lactones with excellent enantioselectivities. Mechanistic studies confirmed the formation of the dienolate intermediates for both catalytic systems. The active ErIII complex is most likely a monomeric species. Interestingly, all lanthanides can catalyze the title reaction, but the efficiency in terms of yield and enantioselectivity depends directly on the radius of the Ln III ion. Similarly, use of the pseudolanthanides ScIII and YIII also resulted in product formation, whereas the larger La III and other transition metal salts, as well as main group metal salts, proved to be inefficient. In addition, various synthetic transformations of 6- CCl3- or 4-silyl-substituted α,β-unsaturated d-lactones, giving access to a number of valuable δ-lactone building blocks, were investigated.
