Tag: M.W=100-150

Ma, XS; Han, YX; Bennett, DJ in [Ma, Xiaoshen; Han, Yongxin; Bennett, David J.] Merck & Co Inc, Dept Discovery Chem, Boston, MA 02115 USA published Selective Synthesis of 1-Dialkylamino-2-alkylbicyclo-[1.1.1]pentanes in 2020, Cited 44. Recommanded Product: 1,4-Dioxa-8-azaspiro[4.5]decane. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

Compared to the abundance of methodologies accessing 1-substituted and 1,3-disubstuted bicyclo[1.1.1] pentanes (BCPs), the synthetic accessibility of BCPs with substitutions at the methylene position has been limited. Herein, we report a selective synthesis of 1-dialkylamino-2-alkylbicyclo[1.1.1]pentanes from prefunctionalized starting materials. We also achieved further functionalizations of these 1,2-disubstituted BCPs and developed a synthesis of these compounds with minimum necessity of chromatographic purifications starting from 1,3-dichloroacetone. Finally, we also detailed the synthesis of a 1,2,3-trisubstituted BCP analogue.

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An article Synthesis of trans-2-Substituted Cyclopropylamines from alpha-Chloroaldehydes WOS:000492114600055 published article about NUCLEOPHILIC CYCLOPROPANATION; ASYMMETRIC CYCLOPROPANATION; 3+2 ANNULATION; AMINO-ACIDS; C-C; BIS(IODOZINCIO)METHANE; AMINOCYCLOPROPANES; CYCLOADDITION; 1,4-ADDITION; HOMOENOLATE in [West, Michael S.; Mills, L. Reginald; McDonald, Tyler R.; Lee, Jessica B.; Ensan, Deeba; Rousseaux, Sophie A. L.] Univ Toronto, Dept Chem, Davenport Res Labs, 80 St George St, Toronto, ON M5S 3H6, Canada; [Lee, Jessica B.] Paraza Pharma Inc, 275 Blvd Armand Frappier, Laval, PQ H7V 4A7, Canada; [Ensan, Deeba] Ontario Inst Canc Res, 661 Univ Ave Suite 510, Toronto, ON M5G 0A3, Canada in 2019, Cited 48. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. Computed Properties of C7H13NO2

Cyclopropylamines are prevalent in pharmaceuticals and agrochemicals. Herein, we report the synthesis of trans-2-substituted cyclopropylamines in high diastereoselectivity from readily available alpha-chloroaldehydes. The reaction proceeds via trapping of an electrophilic zinc homoenolate with an amine followed by ring closure to generate the cyclopropylamine. We have also observed that cyclopropylamine cis/trans-isomerization occurs in the presence of zinc halide salts and that this process can be turned off by the addition of a polar aprotic cosolvent.

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Recently I am researching about C-H FUNCTIONALIZATION; ARYL IODIDES; BOND FUNCTIONALIZATIONS; ARYLATION; PD/NORBORNENE; AMINATION; ALKYLATION; ANILINES; PD; MECHANISM, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [NSF 21472073, 21772075, 21532001]. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Zhang, BS; Li, YK; Gou, XY; Zhang, Z; An, Y; Wang, XG; Liang, YM. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 1,4-Dioxa-8-azaspiro[4.5]decane. Recommanded Product: 177-11-7

This report described the first DMAP and PivOH-promotedortho-C-H amination andipso-allenization reaction of iodobenzenes realized by Pd/norbornene cooperative catalysis. Based on control experiments and DFT calculations, we speculated that the three ligands have different functions and mechanism paths in the reaction.

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An article A Broad-Spectrum Catalytic Amidation of Sulfonyl Fluorides and Fluorosulfates** WOS:000615932400001 published article about SUFEX CLICK CHEMISTRY; NUCLEOPHILIC-SUBSTITUTION; N-ALKYLATION; SULFONAMIDES; ARYL; DISCOVERY; AMINES; ARYLATION; PEPTIDES; REAGENTS in [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, PCFM Lab, Guangzhou 510275, Peoples R China; [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, GDHPRC Lab, Guangzhou 510275, Peoples R China; [Cao, Xiaohui] Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Peoples R China in 2021, Cited 144. Quality Control of 1,4-Dioxa-8-azaspiro[4.5]decane. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

A broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With the activation by the combination of a catalytic amount of 1-hydroxybenzotriazole (HOBt) and silicon additives, amidations of sulfonyl fluorides and fluorosulfates proceeded smoothly and excellent yields were generally obtained (87-99 %). Noticeably, this protocol is particularly efficient for sterically hindered substrates. Catalyst loading is generally low and only 0.02 mol % of catalyst is required for the multidecagram-scale synthesis of an amantadine derivative. In addition, the potential of this method in medicinal chemistry has been demonstrated by the synthesis of the marketed drug Fedratinib via a key intermediate sulfonyl fluoride 13. Since a large number of amines are commercially available, this route provides a facile entry to access Fedratinib analogues for biological screening.

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Authors Tang, SY; Liu, Y; Li, LJ; Ren, XH; Li, J; Yang, GY; Li, H; Yuan, BX in ROYAL SOC CHEMISTRY published article about C-H; OXIDATION; SULFENAMIDES; THIOLS; WATER; STRATEGIES; AMINES; ALKYL; BOND in [Tang, Shanyu; Li, Longjia; Ren, Xuanhe; Li, Jiao; Yang, Guanyu; Li, Heng; Yuan, Bingxin] Zhengzhou Univ, Dept Chem & Mol Engn, Zhengzhou 450001, Henan, Peoples R China; [Liu, Yan] Zhengzhou Univ, Sch Life Sci, Zhengzhou 450001, Henan, Peoples R China in 2019, Cited 44. Application In Synthesis of 1,4-Dioxa-8-azaspiro[4.5]decane. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

A practical and scalable electrochemical oxidation of S-H and N-H was developed. This oxidant-and catalyst-free electrochemical process enables S-N bond formation with inexpensive nickel electrodes in an undivided cell. This procedure exhibits broad substrate scopes and good functional-group compatibility. A 50 g scale oxidative coupling augurs well for industrial applications.

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An article Ni/NHC-catalyzed cross-coupling of methyl sulfinates and amines for direct access to sulfinamides WOS:000498291800009 published article about ASYMMETRIC-SYNTHESIS; COMPLEXES in [Li, Gang-Jian; Pan, You-Lu; Liu, Yan-Ling; Xu, Hai-Feng; Chen, Jian-Zhong] Zhejiang Univ, Coll Pharmaceut Sci, 866 Yuhangtang Rd, Hangzhou, Zhejiang, Peoples R China in 2019, Cited 40. Category: piperidines. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

It was reported to develop a simple and convenient method for the Ni/NHC-catalyzed cross-coupling of methyl sulfinates and amines without an acid/base to afford secondary or tertiary sulfinamides in moderate to good yields. The method can provide the desired products with broad substrate scope, good chemoselectivity and good functional group compatibility. The presented approach may enrich the Nil NHC catalyst system and promote the applications of methyl sulfinates in the organic sulfur chemistry. (C) 2019 Elsevier Ltd. All rights reserved.

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An article Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140) WOS:000460365600004 published article about AGONIST SALVINORIN; PROLACTIN; DYNORPHIN; LY2456302; DOPAMINE; STRESS; 2-METHYL-N-((2′-(PYRROLIDIN-1-YLSULFONYL)BIPHENYL-4-YL)METHYL)PROPAN-1-AMINE; EXPRESSION; DISCOVERY; BINDING in [Guerrero, Miguel; Urbano, Mariangela; Kim, Eun-Kyong; Gamo, Ana M.; Riley, Sean; Abgaryan, Lusine; Leaf, Nora; Brown, Steven J.; Rosen, Hugh; Roberts, Edward] Scripps Res Inst, Dept Mol Med, 10550 North Torrey Pines Rd, La Jolla, CA 92037 USA; [Van Orden, Lori Jean] BlackThorn Therapeut Inc, 780 Brannan St, San Francisco, CA 94103 USA; [Xie, Jennifer Y.; Porreca, Frank] Univ Arizona, Dept Pharmacol, Tucson, AZ 85724 USA; [Cameron, Michael D.] Scripps Res Inst, Dept Mol Med, Jupiter, FL 33458 USA; [Xie, Jennifer Y.] Arkansas State Univ, Coll Osteopath Med, New York Inst Technol, Dept Basic Sci, Jonesboro, AR 72446 USA in 2019, Cited 47. Computed Properties of C7H13NO2. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

kappa opioid receptor (KOR) antagonists are potential pharmacotherapies for the treatment of migraine and stress-related mood disorders including depression, anxiety, and drug abuse, thus the development of novel KOR antagonists with an improved potency/selectivity profile and medication-like duration of action has attracted the interest of the medicinal chemistry community. In this paper, we describe the discovery of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2 H-pyran-4-yl)piperidin-4 amine (CYM-53093, BTRX-335140) as a potent and selective KOR antagonist, endowed with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments. Orally administered CYM-53093 showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice. CYM-53093 exhibited a broad selectivity over a panel of off-target proteins. This compound is in phase 1 clinical trials for the treatment of neuropsychiatric disorders wherein dynorphin is thought to contribute to the underlying pathophysiology.

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Formula: C7H13NO2. Authors De Angelis, L; Crawford, AM; Su, YL; Wherritt, D; Arman, H; Doyle, MP in AMER CHEMICAL SOC published article about in [De Angelis, Luca; Crawford, Alexandra M.; Su, Yong-Liang; Wherritt, Daniel; Arman, Hadi; Doyle, Michael P.] Univ Texas San Antonio, Dept Chem, San Antonio, TX 78249 USA in 2021, Cited 23. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

The formation of nitrile oxides with diazocarbonyl compounds by nitrosyl transfer from tert-butyl nitrite under mild conditions and without the use of a catalyst or an additive is reported. This transformation is broadly applicable to the synthesis of furoxans by dimerization and isoxazoles and isoxazolines by cycloaddition. This methodology is also applied for the millimole-scale synthesis of two biologically active compounds. The formation of the nitrile oxide from a diazoacetamide is stable and confirmed experimentally.

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In 2020 J ORG CHEM published article about ONE-POT SYNTHESIS; N-SULFONYLFORMAMIDINES; SULFONYL AMIDINES; TERTIARY-AMINES; METAL-FREE; INHIBITORS; DESIGN; ROUTE; INTERCEPTION; FORMAMIDINES in [Gou, Quan; Cao, Tuanwu; Tan, Xiaoping; Shi, Wenbing; Ran, Man] Yangtze Normal Univ, Chongqing, Peoples R China; [Liu, Zining; Cheng, Feixiang] Qujing Normal Univ, Qujing, Peoples R China; [Qn, Jun] Yunnan Univ, Kunming, Yunnan, Peoples R China in 2020, Cited 43. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. Product Details of 177-11-7

Herein, we describe an efficient copper-catalyzed coupling of sulfonamides with alkylamines to synthesize (E)-N-sulfonylformamidines. The reaction is accomplished under mild conditions without the use of a corrosive acid or base as an additive. It tolerates a broad scope of substrates and generates the products with exclusive (E)-stereoselectivity.

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In 2019 CHEM COMMUN published article about PALLADIUM-CATALYZED AMINATION; CARBON-SULFUR; COOPERATIVE CATALYSIS; EFFICIENT SYNTHESIS; METAL-COMPLEXES; ACTIVATION; FUNCTIONALIZATION; COBALT; BENZOXAZOLES; CYCLIZATION in [Lv, Zongchao; Wang, Huamin; Quan, Zhicong; Gao, Yuan; Lei, Aiwen] Wuhan Univ, Coll Chem & Mol Sci, Inst Adv Studies, Wuhan 430072, Hubei, Peoples R China; [Lei, Aiwen] Jiangxi Normal Univ, Natl Res Ctr Carbohydrate Synth, Nanchang 330022, Jiangxi, Peoples R China in 2019, Cited 68. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. Category: piperidines

Research on the cleavage of C-C bonds has been well developed. By comparison with this, the activation of C-S bonds remains challenging. Herein, dioxygen-triggered oxidative cleavage of C-S bonds has been achieved, delivering a series of N-containing heterocyclic compounds that are frequently found in pesticides and pharmaceuticals. Additionally, the potential utility of this protocol was further demonstrated by a gram-scale experiment. Mechanistically, dioxygen plays a key role in the cleavage of C-S bonds towards C-N bond formation.

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