Day: October 13, 2022

In 2016,Iwasaki, Takanori; Min, Xin; Fukuoka, Asuka; Kuniyasu, Hitoshi; Kambe, Nobuaki published 《Nickel-Catalyzed Dimerization and Alkylarylation of 1,3-Dienes with Alkyl Fluorides and Aryl Grignard Reagents》.Angewandte Chemie, International Edition published the findings.Recommanded Product: 622-26-4 The information in the text is summarized as follows:

In the presence of a nickel catalyst, 1,3-butadiene undergoes selective dimerization and alkylarylation with alkyl fluorides and aryl Grignard reagents to give 1,6-octadienes with alkyl and aryl groups at the 3- and 8-positions, resp., by the consecutive formation of three carbon-carbon bonds. The formation of an anionic nickel complex plays an important role in forming C-C bonds with alkyl fluorides.2-(Piperidin-4-yl)ethanol(cas: 622-26-4Recommanded Product: 622-26-4) was used in this study.

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Recommanded Product: 622-26-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Richard-Bildstein, Sylvia; Aissaoui, Hamed; Pothier, Julien; Schafer, Gabriel; Gnerre, Carmela; Lindenberg, Eleanor; Lehembre, Francois; Pouzol, Laetitia; Guerry, Philippe. COA of Formula: C10H20N2O2 The article mentions the following:

The chemokine receptor CXCR7, also known as ACKR3, is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies such as neurol. diseases, autoimmune diseases, and cancers. By binding and scavenging the chemokines CXCL11 and CXCL12, CXCR7 regulates their extracellular levels. From an original high-throughput screening campaign emerged an arylketoamide hit among others. The hit-to-lead optimization led to the discovery of a novel chemotype series of acylaminopiperidinecarboxamides. This series provided CXCR7 antagonists that block CXCL11- and CXCL12-induced ss-arrestin recruitment. Further structural modifications on the acylaminopiperidinecarboxamide framework yielded compounds with high CXCR7 antagonistic activities and balanced ADMET properties. The effort described herein culminated in the discovery of ACT-1004-1239 I. Biol. characterization of I demonstrated that it is a potent, insurmountable antagonist. Oral administration of I in mice up to 100 mg/kg led to a dose-dependent increase of plasma CXCL12 concentration In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7COA of Formula: C10H20N2O2)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.COA of Formula: C10H20N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《A Novel Synthesis of Pimavanserin: A Selective Serotonin 5-HT2A Receptor Inverse Agonist》 was written by Hu, Kun; Zhang, Meiju; Wu, Dongdong; Xie, Yuxuan; Ren, Jie. Safety of 1-Methyl-4-piperidone And the article was included in Organic Preparations and Procedures International in 2020. The article conveys some information:

The title compound I was prepared using a novel, low-cost, high-yielding, and eco-friendly procedure starting from (4-hydroxyphenyl)acetic acid. The total yield of I for the 10-step process is 33%. The experimental part of the paper was very detailed, including the reaction process of 1-Methyl-4-piperidone(cas: 1445-73-4Safety of 1-Methyl-4-piperidone)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Safety of 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kang, Zhenghui; Chang, Wenju; Tian, Xue; Fu, Xiang; Zhao, Wenxuan; Xu, Xinfang; Liang, Yong; Hu, Wenhao published their research in Journal of the American Chemical Society in 2021. The article was titled 《Ternary Catalysis Enabled Three-Component Asymmetric Allylic Alkylation as a Concise Track to Chiral α,α-Disubstituted Ketones》.Formula: C10H19NO3 The article contains the following contents:

Herein, a three-component asym. allylation of α-diazo carbonyl compounds with alcs. and allyl carbonates was disclosed by employing a ternary cooperative catalysis of achiral Pd-complex, Rh2(OAc)4, and chiral phosphoric acid CPA. This method represents the first example of three-component asym. allylic alkylation through an SN1-type trapping process, which involves a convergent assembly of two active intermediates, Pd-allyl species and enol derived from onium ylides, providing an expeditious access to chiral α,α-disubstituted ketones in good to high yields with high to excellent enantioselectivity. Combined exptl. and computational studies have shed light on the mechanism of this novel three-component reaction, including the critical role of Xantphos ligand and the origin of enantioselectivity. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Formula: C10H19NO3)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Formula: C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhai, Wenqiang; Lu, Yongping; Zhu, Yabo; Zhou, Mengguang; Ye, Cheng; Shi, Zheng-Zheng; Qian, Wenjian; Hu, Taishan; Chen, Lei published an article in 2021. The article was titled 《Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Category: piperidines The information in the text is summarized as follows:

IRAK4 is a key mediator of innate immunity. There is a high interest in identifying novel IRAK4 inhibitors for the treatment of inflammatory autoimmune diseases. We describe here a highly potent and selective IRAK4 inhibitor HS271 (I) that exhibited superior enzymic and cellular activities, as well as excellent pharmacokinetic properties. HS271 displayed robust in vivo anti-inflammatory efficacy as evaluated in rat models of LPS induced TNFα production and collagen-induced arthritis. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Category: piperidines)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Feng, Baicheng; Dong, Jingjing; Wang, Tielin; Lu, Jianqiang; Jin, Yan published an article in 2021. The article was titled 《Synthesis and characterization of N-(4-(piperidin-4-ylsulfonyl)phenyl)5-vinylpyrimidin-2-amine》, and you may find the article in Indian Journal of Heterocyclic Chemistry.Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate The information in the text is summarized as follows:

Target product N-(4-(piperidin-4-ylsulfonyl)phenyl)5-vinylpyrimidin-2- amine was synthesized using 6-oxopyran-3-carbaldehyde and 4-hydroxypiperidine as starting materials by a series of nucleophilic substitution and oxidation Different acid-binding agents were discussed to explore the effect on the yield of tert-Bu 4-((4-((5-vinylpyrimidin-2-yl)amino)phenyl)sulfonyl)piperidine-1- carboxylate. The structures of products were characterized by 1H NMR and mass spectra. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhang, Zhenhua; Gorski, Bartosz; Leonori, Daniele published an article in 2022. The article was titled 《Merging Halogen-Atom Transfer (XAT) and Copper Catalysis for the Modular Suzuki-Miyaura-Type Cross-Coupling of Alkyl Iodides and Organoborons》, and you may find the article in Journal of the American Chemical Society.Application of 109384-19-2 The information in the text is summarized as follows:

A mechanistically distinct approach to achieve Suzuki-Miyaura-type cross-couplings between alkyl iodides and aryl organoborons was reported. This process required a copper catalyst but, in contrast with previous approaches based on palladium and nickel systems, does not utilizes the metal for the activation of the alkyl electrophile. Instead, this strategy exploited the halogen-atom transfer ability of α-aminoalkyl radicals to convert secondary alkyl iodides into the corresponding alkyl radicals that then were coupled with aryl, vinyl, alkynyl, benzyl and allyl boronate species. These novel coupling reactions feature simple set up and conditions (1 h at room temperature) and facilitate access to privileged motifs targeted by the pharmaceutical sector. In addition to this study using tert-Butyl 4-hydroxypiperidine-1-carboxylate, there are many other studies that have used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application of 109384-19-2) was used in this study.

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Application of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Sakai, Holt A.; MacMillan, David W. C. published an article in 2022. The article was titled 《Nontraditional Fragment Couplings of Alcohols and Carboxylic Acids: C(sp3)-C(sp3) Cross-Coupling via Radical Sorting》, and you may find the article in Journal of the American Chemical Society.Recommanded Product: 109384-19-2 The information in the text is summarized as follows:

In this report, the C(sp3)-C(sp3) cross-coupling of alcs. and carboxylic acids through the dual combination of N-heterocyclic carbene (NHC)-mediated deoxygenation and hypervalent iodine-mediated decarboxylation were described. This mild and practical Ni-catalyzed radical-coupling protocol was employed to prepare a wide array of alkyl-alkyl cross-coupled products, including highly congested quaternary carbon centers from the corresponding tertiary alcs. or tertiary carboxylic acids. Synthetic applications of this methodol. to alc. C1-alkylation and formal homologation, as well as to the late-stage functionalization of drugs, natural products, and biomols. were demonstrated.tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Recommanded Product: 109384-19-2) was used in this study.

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Recommanded Product: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthetic Route of C10H19NO3In 2021 ,《Exploring boron applications in modern agriculture: A structure-activity relationship study of a novel series of multi-substitution benzoxaboroles for identification of potential fungicides》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Liu, Chunliang; Steere, Luke; McGregor, Cari; Frederick, Brittany H.; Pastoor, Timothy; Zhou, Yasheen; Liu, C. Tony; Cai, Yan; Zhou, Haibo; Xu, Musheng; Wang, Jiangong; Kim, Sang Hu; Whitesell, Luke; Cowen, Leah E.; Zhang, Yong-Kang. The article contains the following contents:

Several boron-containing small mols. have been approved by the US FDA to treat human diseases. We explored potential applications of boron-containing compounds in modern agriculture by pursuing multiple research and development programs. Here, we report a novel series of 36 multi-substitution benzoxaboroles (I) wherein R1 is t-Bu, Me, Et, etc.; Z is O, SH, or N; W is O or S; R2 is H; X is H or Cl; Y is H, Me, F or Cl; and R3 is H or Me; a compound class that we recently reported as targeting geranylgeranyl transferase I (GGTase I) and thereby inhibiting protein prenylation (Kim et al., 2020). These compounds were designed, synthesized, and tested against the agriculturally important fungal pathogens Mycosphaerella fijiensis and Colletotrichum sublineolum in a structure-activity relationship study. Compounds Pr (7-chloro-1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)carbamate, benzyl (7-chloro-1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)carbamate, 4-chlorobenzyl (7-chloro-1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)carbamate, O-(4-chlorobenzyl) (7-chloro-1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)carbamothioate and O-(4-fluorobenzyl) (7-chloro-1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)carbamothioate were identified as active leads with excellent antifungal MIC95 values in the range of 1.56-3.13 ppm against M. fijiensis and 0.78-3.13 ppm against C. sublineolum. The experimental process involved the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Synthetic Route of C10H19NO3)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Synthetic Route of C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《A practical method for functionalized peptide or amide bond formation in aqueous-ethanol media with EDC as activator》 was written by Pu, Yangwei John; Vaid, Radhe K.; Boini, Sathish K.; Towsley, Robert W.; Doecke, Christopher W.; Mitchell, David. Category: piperidines And the article was included in Organic Process Research & Development on April 30 ,2009. The article conveys some information:

Selective formation of amides or peptides with ethanol as solvent using a convenient one-pot procedure in which acid activating agent N-(3-dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride (EDC) is simply added to a mixture of the carboxylic acid, amine, catalytic HOBt (1-hydroxy benzotriazole), and NMM (N-methylmorpholine) as base has been developed. Sensitive functionalities such as hydroxyl groups are well tolerated under the reaction conditions. In addition, isolation of products is usually by simple filtration from the reaction media. The scope and generality of this methodol. was investigated. The experimental part of the paper was very detailed, including the reaction process of 1-(Piperidin-4-yl)-1H-indole(cas: 118511-81-2Category: piperidines)

1-(Piperidin-4-yl)-1H-indole(cas: 118511-81-2) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem