Month: October 2022

On January 31, 2020, Miao, Xiuqi; Xing, Lingyun; Guo, Ming; Zhang, Hong; Liu, Sicong; Yin, Shiliang; Gong, Ping; Zhang, Dajun; Zhai, Xin published an article.Application In Synthesis of 2-Chloroacetamide The title of the article was Design, synthesis and biological evaluation of 2-arylaminopyrimidine derivatives bearing 1,3,8-triazaspiro[4,5]decan-4-one or piperidine-3-carboxamide moiety as novel Type-I1/2 ALK inhibitors. And the article contained the following:

Aiming to develop novel Type-I1/2 inhibitors of ALK to overcome extensive resistance mutations, especially the L1196M mutation surrounding the ATP pocket, two series of 2-arylaminopyrimidine derivatives (I (R1 = pyrrolidin-1-yl, piperidin-1-yl, 4-methylpiperazin-1-yl, 4-(2-hydroxyethyl)piperazin-1-yl), II (R2 = 4-methylpiperazin-1-yl, 4-(2-hydroxyethyl)piperazin-1-yl) and III (R3 = ethoxycarbonylmethylamino, 2-(piperidin-1-yl)acetamido, 2-(4-methylpiperazin-1-yl)acetamido, etc.), IV (R4 = allyl, cyclopropanecarbonyl, 2-carboxyethyl, etc.)) were designed based on scaffold hopping. The extensive structural elaboration discovered compound IV ((A), R4 = 3-ethoxy-3-oxopropyl) which possessed excellent IC50 values of 0.06 and 0.23μM against ALK-pos. Karpas299 and H2228 cell lines, resp. Meanwhile, (A) displayed encouraging inhibitory potency in the ALKWT (2.5 nM) and ALKL1196M (6.5 nM) enzymic assays. Furthermore, the AO/EB and Hoechst 33258 assays illustrated that (A) could induce cell apoptosis in a dose-dependent manner. Eventually, the mol. docking of (A) with ALK clearly presented the vital interactions within the active site, which was in accordance with Type-I1/2 inhibitor binding mode. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Application In Synthesis of 2-Chloroacetamide

The Article related to arylaminopyrimidine triazaspirodecanone preparation alk inhibitor antitumor docking, piperidine carboxamide arylaminopyrimidine preparation alk inhibitor antitumor docking, imidazolidin-2-one, l1196m mutants, piperidine-3-carboxamide, type-i(1/2) alk inhibitor and other aspects.Application In Synthesis of 2-Chloroacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Cai, Bao-Gui; Li, Qian; Zhang, Qiong; Li, Lei; Xuan, Jun published an article in 2021, the title of the article was Synthesis of trisubstituted hydroxylamines by a visible light-promoted multicomponent reaction.Related Products of 102-07-8 And the article contains the following content:

A green and efficient method for the synthesis of trisubstituted hydroxylamines I [R1 = H, Me, F, etc.; R2 = Me, iPr, tBu, admantyl; R3 = Me, cyclopentyl, methylallyl, etc.; Ar = Ph, 2-naphthyl, 4-MeC6H4, etc.] via three component reaction of β-keto esters, 2-nitrosopyridine and aryldiazoacetates was developed. Also, trisubstituted hydroxylamines II [R4 = H, Me, Br, etc.; R5 = Me, iPr, tBu, admantyl; R6 = Me, cyclopentyl, methylallyl, etc.; Ar1 = Ph, 4-MeOC6H4, 4-ClC6H4, etc.] were developed via multicomponent reaction of β-keto esters, 2-nitrosopyridine, cyclic ethers and aryldiazoacetates. Both reactions were occurred under sole blue LED irradiation in the absence of addnl. catalysts and additives. Two different kinds of trisubstituted hydroxylamines I and II could be easily obtained by simply changing the reaction media used. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Related Products of 102-07-8

The Article related to trisubstituted hydroxylamine green preparation, keto ester nitrosopyridine diazoacetate three component visible light promoted, hydroxylamine trisubstituted green preparation, ester nitrosopyridine diazoacetate cyclic ether multicomponent visible light promoted and other aspects.Related Products of 102-07-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On May 15, 2020, Parasram, Marvin; Shields, Benjamin J.; Ahmad, Omar; Knauber, Thomas; Doyle, Abigail G. published an article.Recommanded Product: 5455-98-1 The title of the article was Regioselective Cross-Electrophile Coupling of Epoxides and (Hetero)aryl Iodides via Ni/Ti/Photoredox Catalysis. And the article contained the following:

A cross-electrophile coupling reaction of epoxides and (hetero)aryl iodides that operates via the merger of three catalytic cycles involving a Ni-, Ti-, and organic photoredox catalyst has been developed. Three distinct classes of epoxides, styrene oxides, cyclic epoxides, and terminal aliphatic epoxides, underwent coupling in moderate to good yield and high regioselectivity with the use of three different nitrogen-based ligands for Ni under otherwise identical reaction conditions. The mild reaction conditions accommodate a broad scope of abundant and complex coupling partners. Mechanistic studies suggest that when styrene oxides are employed radical intermediates are involved via Ti-radical ring opening of the epoxide. Conversely, for terminal aliphatic epoxides, involvement of an iodohydrin intermediate enables the formation of the unexpected linear product. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Recommanded Product: 5455-98-1

The Article related to arylalkyl alc regioselective preparation, epoxide hetero aryl iodide cross electrophile coupling photoredox catalyst, arylation, cross-electrophile coupling, epoxides, nickel catalysis, photochemistry, photoredox catalysis, radical chemistry, titanium catalysis and other aspects.Recommanded Product: 5455-98-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 18, 2019, Hardy, Jeanne A.; Meka, Penchala Narasimhara published a patent.Formula: C9H10N2O The title of the patent was Preparation of furoxan-based compounds for treating neurodegenerative diseases. And the patent contained the following:

This invention relates to the title compounds I [R1 = H or aryl; R2 = H or aryl; X1 and X2 = (independently) N, N+-O- or CR3 (wherein R3 = H or alkyl and only one of X1 and X2 can be N+-O-); with the proviso] or pharmaceutically acceptable salts, polymorphs, prodrugs, solvates or clathrates thereof, as well as to pharmaceutical compositions comprising such compounds, and to methods for using such compounds/pharmaceutical compositions for treating neurodegenerative diseases including Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, and multiple sclerosis (MS). Over fifty compounds I were prepared E.g., a multi-step synthesis of II, starting from cyclohexanone, was described. A method for inhibiting caspase-6 with a compound that reacts with the sulhydryl group (SH) on cysteine 246 of caspase-6 was disclosed (no biol. data given). The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Formula: C9H10N2O

The Article related to furoxan derivative preparation neurodegenerative alzheimer’s parkinson’s huntington’s disease treatment, caspase 6 inhibitor furoxan derivative triazolobenzooxadiazole preparation, multiple sclerosis treatment furoxan derivative triazolobenzooxadiazole preparation and other aspects.Formula: C9H10N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On February 28, 2018, Sapegin, Alexander; Kalinin, Stanislav; Angeli, Andrea; Supuran, Claudiu T.; Krasavin, Mikhail published an article.Recommanded Product: 97-09-6 The title of the article was Unprotected primary sulfonamide group facilitates ring-forming cascade en route to polycyclic [1,4]oxazepine-based carbonic anhydrase inhibitors. And the article contained the following:

4-Chloro-3-nitrobenzenesulfonamide reacted cleanly at room-temperature with a range of bis-electrophilic phenols bearing an NH-acidic functionality (secondary carboxamide or pyrazole) in the ortho-position. This produced a novel class of [1,4]oxazepine-based primary sulfonamides which exhibited strong inhibition of therapeutically relevant human carbonic anhydrases. 2-Chloronitrobenzene did not enter a similar cyclocondensation process, even under prolonged heating. Thus, the primary sulfonamide functionality plays a dual role by enabling the [1,4]oxazepine ring construction and acting as a enzyme prosthetic zinc-binding group when the resulting [1,4]oxazepine sulfonamides are employed as carbonic anhydrase inhibitors. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Recommanded Product: 97-09-6

The Article related to oxazepine primary sulfonamide preparation human carbonic anhydrase inhibitor, carbonic anhydrase inhibitors, electron-withdrawing group, isoform-selectivity, nucleophilic aromatic substitution, primary sulfonamide, reactivity-matched substrates, smiles rearrangement and other aspects.Recommanded Product: 97-09-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Mao, Yu; Liu, Yeqing; Yu, Lei; Ni, Shengyang; Wang, Yi; Pan, Yi published an article in 2021, the title of the article was Uranyl-catalysed C-H alkynylation and olefination.Product Details of 685-91-6 And the article contains the following content:

A strategy to utilize uranyl for direct alkynylation and olefination of amides was described. The uranyl cation (UO22+) was identified as a highly oxidizing agent to abstract hydrogen atoms from C-H bonds for the formation of carbon-centered radicals. The photoexcitation of uranyl cations provides a range of carbon-centered radicals via hydrogen atom transfer, which can be successfully applied in cross-coupling reactions with a broad range of alkynyl and alkenyl bromides. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Product Details of 685-91-6

The Article related to amide bromoalkyne uranyl catalyst regioselective alkynylation, alkynyl amide preparation, alkenylbromide amide uranyl catalyst regioselective alkenylation, alkenyl amide preparation, allylbromide amide uranyl catalyst regioselective allylation, allyl amide preparation and other aspects.Product Details of 685-91-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On March 22, 2021, Hu, Zhiyong; Wei, Xiao-Jing; Handelmann, Jens; Seitz, Ann-Katrin; Rodstein, Ilja; Gessner, Viktoria H.; Goossen, Lukas J. published an article.SDS of cas: 685-91-6 The title of the article was Coupling of Reformatsky reagents with aryl chlorides enabled by ylide-functionalized phosphine ligands. And the article contained the following:

The coupling of aryl chlorides with Reformatsky reagents is a desirable strategy for the construction of α-aryl esters but has so far been substantially limited in the substrate scope due to many challenges posed by various possible side reactions. This limitation has now been overcome by the tailoring of ylide-functionalized phosphines to fit the requirements of Negishi couplings. Record-setting activities were achieved in palladium-catalyzed arylations of organozinc reagents with aryl electrophiles using a cyclohexyl-YPhos ligand bearing an ortho-tolyl-substituent in the backbone. This highly electron-rich, bulky ligand enables the use of aryl chlorides in room temperature couplings of Reformatsky reagents. The reaction scope covers diversely functionalized arylacetic and arylpropionic acid derivatives Aryl bromides and chlorides can be converted selectively over triflate electrophiles, which permits consecutive coupling strategies. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).SDS of cas: 685-91-6

The Article related to aryl ester synthesis steric hindrance natural product drug, reformatsky reagent negishi coupling aryl chloride ylide phosphine ligand, arylation catalyst palladium aryl bromide chloride, reformatsky reagent, aryl chlorides, cross-coupling, phosphine ligands, selectivity and other aspects.SDS of cas: 685-91-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On November 1, 2022, Wang, Juanqiang; Zhao, Wentao; Guo, Wenping; Li, Yingying; Jiang, Rui; Li, Huichen; Wang, Shouwei; Li, Zhigang published an article.Application of 144-80-9 The title of the article was Simultaneous screening and analysis of 155 veterinary drugs in livestock foods using ultra-high performance liquid chromatography tandem quadrupole linear-ion-trap mass spectrometry. And the article contained the following:

Veterinary drugs are widely used to improve the health and growth of livestock. The supervision of these residues is necessary to ensure food safety. A high-throughput method based on Oasis PRiME HLB with solid phase extraction for simultaneous qual. and quant. anal. of 155 veterinary drugs in livestock foods was developed by the ultra-high performance liquid chromatog. tandem quadrupole linear-ion-trap mass spectrometry (UHPLC-QTRAP-MS). The limits of detection and quantification ranged from 0.5 μg/kg to 5 μg/kg and 2 μg/kg to 20 μg/kg, resp. For over 85% of the analytes, the recoveries were between 60% and 120%. The pos. simulated samples perfectly matched with a purity fit value over 70% from the self-built library. The screening results of UHPLC-QTRAP-MS were almost consistent with UHPLC tandem quadrupole-exactive orbitrap mass spectrometry (UHPLC-Q-Exactive Orbitrap/MS). The evaluated UHPLC-QTRAP-MS method was powerful and reliable for the screening and quantification of veterinary drugs in real samples. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Application of 144-80-9

The Article related to livestock food veterinary drug ultra high performance liquid chromatog, livestock foods, multi-residue analysis, qualitative screening, quantitative analysis, ultra-high performance liquid chromatography tandemquadrupole linear-ion-trap mass spectrometry, veterinary drugs and other aspects.Application of 144-80-9

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On October 12, 2000, Matsubara, Koki; Kida, Hitoshi published a patent.HPLC of Formula: 167316-28-1 The title of the patent was Method for the preparation of tricyclic amino alcohol derivatives through azides. And the patent contained the following:

Tricyclic amino alc. derivatives represented by general formula [I; wherein R1 is lower alkyl or benzyl; *1 represents an asym. carbon atom; R2 is hydrogen, halogeno or hydroxyl; and A is a substituent represented by general formula Q or Q1 (wherein X is NH, O, or S; R5 is hydrogen, hydroxyl, amino, or acetylamino; and *2 represents an asym. carbon atom when R5 is not hydrogen)] are prepared via asym. reduction of phenacyl azides (II; R21 is hydrogen, halogeno or (un)protected hydroxyl; R3 is hydrogen or amino-protecting group; and R1 is lower alkyl or benzyl) to chiral azido alcs. (III) or amino alcs. (IV; R21, R1, R3 are same as above). This process makes it possible to prepare the derivatives I by a short, easy, inexpensive, and practical production process excellent in industrial workability. Compounds I are useful in the treatment and prevention of diabetes, obesity, hyperlipidemia, and so on (no data). Thus, 58 mg [(S,S)-N-methanesulfonyl-1,2-diphenylethylenediamine](p-cymene)ruthenium (preparation given) was added to a solution of 3.6 g 2-azido-1-(4-benzyloxy-3-methylsulfonylaminophenyl)ethanone (preparation given) in 2.5 mL formic acid/triethylamine solution (Fluka) in 6.5 mL THF and stirred at 5° for 43 h to give 95.0% (R)-2-azido-1-(4-benzyloxy-3-methylsulfonylaminophenyl)ethanol (94.2 %e.e.). In another example, 2-amino-1-(4-benzyloxy-3-methylsulfonylaminophenyl)ethanone hydrochloride (1.0 g) and 2 μL Et3N were added to a solution of 133 mg chloro(1,5-cyclooctadiene)rhodium(II) dimer and 397 mg (2R,4R)-N-(tert-butoxycarbonyl)-4-dicyclohexylphosphino-2-diphenylphosphinopyrrolidine and stirred under hydrogen atm. at room temperature for 24 h to give 94.0% (R)-2-amino-1-(4-benzyloxy-3-methylsulfonylaminophenyl)ethanol (V). Reductive benzylation of V with benzaldehyde in the presence of Pt2O under hydrogen atm. at room temperature for 15 h followed by amidation with (9H-carbazol-2-yloxy)acetic acid using DCC in THF at room temperature for 24 h, borane reduction in THF, and hydrogenolysis over 10% Pd-C in MeOH gave (R)-2-[N-[2-(9H-carbazol-2-yloxy)]ethyl]amino-1-(4-hydroxy-3-methylsulfonylaminophenyl)ethanol. The experimental process involved the reaction of N-[(1S,2S)-2-Amino-1,2-diphenylethyl]-1,1,1-trifluoromethanesulfonamide(cas: 167316-28-1).HPLC of Formula: 167316-28-1

The Article related to tricyclic amino alc preparation treatment diabetes obesity hyperlipidemia, asym reduction phenacyl azide, ruthenium complex asym reduction catalyst, carbazolyloxyethylaminophenylethanol preparation antidiabetic, phenylethanolamine carbazolyloxyethyl preparation antidiabetic and other aspects.HPLC of Formula: 167316-28-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Jain, Isha; Sharma, Ramandeep; Malik, Payal published an article in 2019, the title of the article was Manganese-mediated acetylation of alcohols, phenols, thiols, and amines utilizing acetic anhydride.Application of 685-91-6 And the article contains the following content:

Manganese(II) chloride-catalyzed acetylation of alcs., phenols, thiols and amines RXH (R = Ph, n-octyl, cyclohexyl, etc.; X = O, S, NH), morpholine with acetic anhydride is reported. This method is environment-friendly and economically viable as it involves inexpensive, relatively benign catalyst, mild reaction condition, and simple workup. Acetylation is performed under the solvent-free condition at ambient temperature and acetylated products RXAc, N-acetylmorpholine obtained in good to excellent yields. Primary, secondary heterocyclic amines, and phenols with various functional groups are smoothly acetylated in good yields. This method exhibits exquisite chemoselectivity, and the amino group is preferentially acetylated in the presence of a hydroxyl/thiol group. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Application of 685-91-6

The Article related to acetate preparation green chem solventless, aliphatic alc acetic anhydride acetylation manganese catalyst, phenol acetic anhydride acetylation manganese catalyst, thiophenol acetic anhydride acetylation manganese catalyst, aniline acetic anhydride acetylation manganese catalyst and other aspects.Application of 685-91-6

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics