Month: November 2022

Jain, Shubha; Reddy, B. Nagi; Rao, K. Sambasiva; Neeliah, G. published an article in 2010, the title of the article was Microwave assisted synthesis of indole substituted alkenes using Knoevenagel condensation reaction and their antibacterial activity study.Computed Properties of 75629-62-8 And the article contains the following content:

The reaction rate of the Knoevenagel condensation can be dramatically enhanced by irradiating the reaction mixture containing an 3-indolealdehyde, active methylene compound, L-proline and PhCl using a com. microwave oven. Several Knoevenagel condensation products were synthesized within 5-17 min in good yields. The new compounds were also screened for antibacterial activity. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).Computed Properties of 75629-62-8

The Article related to indole active methylene knoevenagel condensation microwave, indolyl alkene preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 75629-62-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Elslager, Edward F.; Jacob, Patricia; Werbel, Leslie M. published an article in 1972, the title of the article was Antimalarial drugs. 28. Folate antagonists. 6. Synthesis and antimalarial effects of fused 2,4-diaminothieno [2,3-d] pyrimidines.Category: nitriles-buliding-blocks And the article contains the following content:

2,4-Diamino-5,7 – dihydro – 6H – thiopyrano[4 ,3 :4,5]thieno[2,3-d]pyrimidine, 2,4-diamino-9H-indeno[1 ,2 :4,5]thieno[2,3-d]-pyrimidine, 2,4-diamino – 5H – indeno[2 ,1 :4,5]thieno[2,3 – d]-pyrimidine, 9,11-diamino-5,6-dihydronaphtho[1 ,2 :4,5]thieno-[2,3-d]pyrimidine, 7,9-diamino-5,6-dihydronaphtho[2 ,1 :4,5]-thieno[2,3-d]pyrimidine, 2,4-diamino – 7 – benzyl – 5,6,7,8 – tetrahydropyrido[4 ,3 :4,5]thieno[2,3-d]pyrimidine, and various 2,4-diamino – 5,6,7,8 – tetrahydro – [1]benzothieno[2,3 – d]pyrimidines were prepared by cyclization of the requisite fused 2-aminothiophene-3-carbonitriles with ClC(:NH)Nh2.HCl. Several compounds exhibited strong inhibitory effects against Streptococcus faecalis (MGH-2), Staphylococcus aureus (UC-76), Streptococcus faecalis (ATCC 8043), Lactobacillus casei (ATCC 7469), and Pediococcus cerevisiae (ATCC 8081) in vitro, and three compounds displayed slight antimalarial activity against Plasmodium berghei in mice and Plasmodium falciparum (Uganda I) in vitro. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Category: nitriles-buliding-blocks

The Article related to thienopyrimidine diamino fused, antimalarial fused diaminothienopyrimidine, antibacterial fused diaminothienopyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: nitriles-buliding-blocks

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On February 25, 2018, Tuo, Wei; Bollier, Melanie; Leleu-Chavain, Natascha; Lemaire, Lucas; Barczyk, Amelie; Dezitter, Xavier; Klupsch, Frederique; Szczepanski, Fabien; Spencer, John; Chavatte, Philippe; Millet, Regis published an article.Electric Literature of 5098-14-6 The title of the article was Development of novel oxazolo[5,4-d]pyrimidines as competitive CB2 neutral antagonists based on scaffold hopping. And the article contained the following:

A series of novel oxazolo[5,4-d]pyrimidines I [R1 = H, Cl, F, CF3; R2 = H, Me; R3 = n-Bu, cyclohexylmethyl, 1-methylpiperazinyl, etc.] was designed via a scaffold hopping strategy and synthesized through a newly developed approach. All these compounds I were evaluated for their biol. activity toward CB1/CB2 cannabinoid receptors, their metabolic stability in mice liver microsomes and their cytotoxicity against several cell lines. Eight compounds I [R1 = Cl, CF3; R2 = H, Me; R3 = 1-methylpiperazinyl, 1-ethylpiperazinyl, 1-acetylpiperazinyl] were identified as CB2 ligands with Ki values less than 1 ΜM. It was noteworthy that compounds I [R1 = Cl; R2 = Me; R3 = 1-methylpiperazinyl, 1-ethylpiperazinyl] showed CB2 binding affinity in the nanomolar range and significant selectivity over CB1 receptors. Interestingly, functionality studies imply that they behaved as competitive neutral antagonists. Moreover, all tested compounds I were devoid of cytotoxicity toward several cell lines, including Chinese hamster ovary cells (CHO) and human colorectal adenocarcinoma cells HT29. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Electric Literature of 5098-14-6

The Article related to oxazolopyrimidine preparation cytotoxicity sar cannabinoid receptor antagonist, cb(2) receptor, cannabinoid, neutral antagonist, oxazolo[5,4-d]pyrimidine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 5098-14-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Lega, D. A.; Chernykh, V. P.; Shemchuk, L. A. published an article in 2016, the title of the article was The study of the three-component interaction between 1-ethyl-1H-2,1-benzothiazin-4(3H)-one 2,2 dioxide, hetarylcarbaldehydes and active methylene nitriles.HPLC of Formula: 75629-62-8 And the article contains the following content:

Some peculiarities of the three-component reaction of 1-ethyl-1H-2,1-benzothiazin-4(3H)-one 2,2-dioxide with active methylene nitriles and hetarylcarbaldehydes have been described in this article. It has been found that if malononitrile is used, the products of the three-component reaction are 2-amino-4-hetaryl-3-cyano-6-ethyl-4,6- dihydropyrano[3,2-c][2,1]benzothiazine 5,5-dioxides irresp. of the hetaryl fragment nature in the initial aldehyde. When using Et cyanoacetate as an active methylene nitrile instead of malononitrile the reaction lost its selectivity. In this case, depending on the hetarylcabaldehyde, three different types of products were obtained, namely, 2-amino-3-alkoxycarbonyl-4-hetaryl-4H-pyrans (for pyridine-3-, pyridine-4-carbaldehydes, and furan-2-carbaldehyde), triethylammonium salt of bis(1-ethyl-1H-2,1-benzothiazin-2,2- dioxo-4-ol-3-yl)(2-thienyl)methane (for thiophen-2-carbaldehyde) or Et 2-cyano-3-(1H-indol-3-yl)acrylate (for indole-3-carbaldehyde). Formation of a stable triethylammonium salts was considered as the process competitive with formation of 2-amino-4H-pyrans. This has allowed us to propose the modified mechanism of 2-amino-4H-pyran formation. This mechanism includes formation of triethylammonium salts of bis-adducts. According to this mechanism 2-amino-3-ethoxycarbonyl-4-(2-thienyl)-4H-pyran without any impurity of bis-adduct could be selectively obtained using the three-component reaction. Triethylammonium salts of bis-adducts were obtained by direct reaction of 1-ethyl-1H-2,1-benzothiazin-4(3H)-one 2,2-dioxide with hetarylcarbaldehydes in the presence of equimolar amounts of triethylamine. It has been shown that the three-component reaction of 1-ethyl-1H-2,1-benzothiazM(3H)-one 2,2-dioxide with active methylene nitriles and hetarylcarbaldehydes is a more effective tool for obtaining fused 2-amino-4-hetaryl-4H-pyrans compared to the stepwise approach. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).HPLC of Formula: 75629-62-8

The Article related to three component reaction ethylbenzothiazinone dioxide hetarylcarbaldehyde nitrile, Physical Organic Chemistry: Ring Formation, Cleavage, Enlargement, and Contraction and other aspects.HPLC of Formula: 75629-62-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On August 5, 2021, Lamotte, Yann; Dodic, Nerina; Tap, Aurelien; Denis, Alexis; Brusq, Jean-Marie; Daoubi Khamlichi, Mourad; Benderitter, Pascal Andre Rene published a patent.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile The title of the patent was Preparation of macrocyclic RIP2-kinase inhibitors. And the patent contained the following:

The invention relates to macrocyclic compounds of formula I and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2-kinase, and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the invention provides methods of using said compounds, for instance as a medicine or diagnostic agent. Compounds of formula I, wherein R1 is halo, alkynyl, CN, etc.; R2 and R10 are independently H and halo; R3, R3′, R4, R4′, R7 and R8 are independently H and C1-6 alkyl; R5 is OH, halo, CN, etc.; R6 is H, halo, C1-6 alkyl, etc.; R9 is H, C1-6 alkyl, COC1-6alkyl, etc.; and stereoisomers, tautomers, racemates, salts, hydrates, N-oxide forms, and solvates thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their RIP-2 kinase inhibitory activities (some data given). The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

The Article related to macrocycle rip2 kinase inhibitor preparation diagnostic treatment, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Application In Synthesis of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On May 31, 2020, Vitkovska, Viktorija; Zogota, Rimants; Kalnins, Toms; Zelencova, Diana; Suna, Edgars published an article.Computed Properties of 5098-14-6 The title of the article was Aliphatic chain-containing macrocycles as diazonamide A analogs. And the article contained the following:

Aliphatic alkyl chain-containing 12-14-membered macrocycles were designed as structural analogs of antimitotic natural product diazonamide A. Macrocycles were synthesized from 5-bromooxazole in 7 to 9 linear steps using Ru-catalyzed ring-closing metathesis as the key transformation. Heat effect of binding to α,β-tubulin tetramer (T4-RB3 complex) has been measured for the synthesized macrocycles by isothermal titration calorimetry method. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Computed Properties of 5098-14-6

The Article related to diazonamide a analog aliphatic chain macrocycle preparation dissociation constant, Heterocyclic Compounds (More Than One Hetero Atom): Eight- and Higher-Membered Rings and other aspects.Computed Properties of 5098-14-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Chen, Hui; Zhao, Sihan; Cheng, Shaobing; Dai, Xingjie; Xu, Xiaoying; Yuan, Weicheng; Zhang, Xiaomei published an article in 2019, the title of the article was Synthesis of Novel Pterocarpen Analogues via [3 + 2] Coupling-Elimination Cascade of α,α-Dicyanoolefins with Quinone Monoimines.Related Products of 2510-01-2 And the article contains the following content:

By employing triethylamine as a catalyst, [3+2]-coupling-elimination cascade of α,α-dicyano-olefins, e.g., I, with quinone monoimines, e.g., II, was realized. The reactions afforded various novel pterocarpen analogs, e.g., III, with generally moderate yields (up to 75%). In addition, a plausible reaction mechanism was proposed. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Related Products of 2510-01-2

The Article related to pterocarpen analog preparation coupling elimination cascade triethylamine catalyst, Biomolecules and Their Synthetic Analogs: Flavonoids and Natural and Fused Coumarins and other aspects.Related Products of 2510-01-2

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On April 12, 2004, Blazej, Sylwia; Kwast, Andrzej; Makosza, Mieczyslaw published an article.Reference of 3-Chloro-4-nitrobenzonitrile The title of the article was cine-Substitution of the nitro group in 2,4-disubstituted nitroarenes with carbanions of aryl alkyl sulfones. And the article contained the following:

Rapid protonation of short lived σH adducts, e.g., I, derived from the nucleophilic addition of aryl alkyl sulfones to 2,4-disubstituted nitrobenzenes, resulted in elimination of nitrous acid giving 1,3,5-trisubstituted benzenes, e.g., II, as products of cine-substitution of the nitro group. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Reference of 3-Chloro-4-nitrobenzonitrile

The Article related to nitrobenzene aryl alkyl sulfone cine substitution, aryl arylalkyl sulfone preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Sulfoxides and Sulfones and other aspects.Reference of 3-Chloro-4-nitrobenzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On May 27, 2021, Shen, Chunli; Sun, Guanglong; Wu, Chengde; Chen, Shuhui published a patent.Reference of 5-Bromo-3-hydroxypicolinonitrile The title of the patent was Bicyclic compound used as selective androgen receptor modulator. And the patent contained the following:

Disclosed are a bicyclic compound used as a non-steroidal selective androgen receptor modulator and the use thereof in the preparation of a drug for treating related diseases which are mediated by an androgen receptor. Specifically, the present invention discloses a compound as shown in formula I or a pharmaceutically acceptable salt thereof. The experimental process involved the reaction of 5-Bromo-3-hydroxypicolinonitrile(cas: 1160936-51-5).Reference of 5-Bromo-3-hydroxypicolinonitrile

The Article related to bicyclic compound preparation androgen receptor modulator treatment disease, Alicyclic Compounds: Bicyclic Compounds, Including Azulenes, Heptalenes, and Pentalenes and other aspects.Reference of 5-Bromo-3-hydroxypicolinonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Liu, Yingtian; Dang, Xinxin; He, Yu; Bai, Hudong; Chen, Xuehong; Li, Jun-Long; Fan, Junting; Jiang, Hezhong; Li, Jiahong published an article in 2019, the title of the article was Synthesis of 2-cyanoacrylamides through Pd-catalyzed monohydration of methylenemalononitriles.Recommanded Product: 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile And the article contains the following content:

A straightforward and efficient method was developed for the synthesis of 2-cyanoacrylamides R1R2C:C(CN)CONH2 [R1 = n-Pr, Ph, 4-MeOC6H4, PhCH:CH, 2-furyl, etc., R2 = H; R1 = Ph, R2 = Me, Ph; R1R2 = (CH2)5, o-C6H4CH2CH2, etc.] from 2-methylenemalononitriles R1R2C:C(CN)2 in good to excellent yields through monohydration under mild and simple reaction conditions. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Recommanded Product: 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile

The Article related to methylene malononitrile preparation diastereoselective monohydration palladium catalyst, cyano acrylamide preparation, Aliphatic Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Recommanded Product: 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts