Category: 405057-75-2

Cox, Christopher D.’s team published research in Journal of Medicinal Chemistry in 2008 | CAS: 405057-75-2

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Recommanded Product: 405057-75-2

Cox, Christopher D.; Coleman, Paul J.; Breslin, Michael J.; Whitman, David B.; Garbaccio, Robert M.; Fraley, Mark E.; Buser, Carolyn A.; Walsh, Eileen S.; Hamilton, Kelly; Schaber, Michael D.; Lobell, Robert B.; Tao, Weikang; Davide, Joseph P.; Diehl, Ronald E.; Abrams, Marc T.; South, Vicki J.; Huber, Hans E.; Torrent, Maricel; Prueksaritanont, Thomayant; Li, Chunze; Slaughter, Donald E.; Mahan, Elizabeth; Fernandez-Metzler, Carmen; Yan, Youwei; Kuo, Lawrence C.; Kohl, Nancy E.; Hartman, George D. published an article in Journal of Medicinal Chemistry. The title of the article was 《Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer》.Recommanded Product: 405057-75-2 The author mentioned the following in the article:

Inhibition of kinesin spindle protein (KSP) is a novel mechanism for treatment of cancer with the potential to overcome limitations associated with currently employed cytotoxic agents. Herein, we describe a C2-hydroxymethyl dihydropyrrole KSP inhibitor (11) that circumvents hERG channel binding and poor in vivo potency, issues that limited earlier compounds from our program. However, introduction of the C2-hydroxymethyl group caused 11 to be a substrate for cellular efflux by P-glycoprotein (Pgp). Utilizing knowledge garnered from previous KSP inhibitors, we found that β-fluorination modulated the pKa of the piperidine nitrogen and reduced Pgp efflux, but the resulting compound (14) generated a toxic metabolite in vivo. Incorporation of fluorine in a strategic, metabolically benign position by synthesis of an N-methyl-3-fluoro-4-(aminomethyl)piperidine urea led to compound 30 that has an optimal in vitro and metabolic profile. Compound 30 (MK-0731) was recently studied in a phase I clin. trial in patients with taxane-refractory solid tumors. The experimental part of the paper was very detailed, including the reaction process of 1-Cbz-4-Methylaminopieridine(cas: 405057-75-2Recommanded Product: 405057-75-2)

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Recommanded Product: 405057-75-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Blizzard, Timothy A.’s team published research in Bioorganic & Medicinal Chemistry Letters in 2014 | CAS: 405057-75-2

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Reference of 1-Cbz-4-Methylaminopieridine

Blizzard, Timothy A.; Chen, Helen; Kim, Seongkon; Wu, Jane; Bodner, Rena; Gude, Candido; Imbriglio, Jason; Young, Katherine; Park, Young-Whan; Ogawa, Aimie; Raghoobar, Susan; Hairston, Nichelle; Painter, Ronald E.; Wisniewski, Doug; Scapin, Giovanna; Fitzgerald, Paula; Sharma, Nandini; Lu, Jun; Ha, Sookhee; Hermes, Jeff; Hammond, Milton L. published an article on February 1 ,2014. The article was titled 《Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Reference of 1-Cbz-4-Methylaminopieridine The information in the text is summarized as follows:

β-Lactamase inhibitors with a bicyclic urea core and a variety of heterocyclic side chains were prepared and evaluated as potential partners for combination with imipenem to overcome class A and C β-lactamase mediated antibiotic resistance. The piperidine analog 3 (MK-7655) inhibited both class A and C β-lactamases in vitro. It effectively restored imipenem’s activity against imipenem-resistant Pseudomonas and Klebsiella strains at clin. achievable concentrations A combination of MK-7655 and Primaxin is currently in phase II clin. trials for the treatment of Gram-neg. bacterial infections. In the experiment, the researchers used many compounds, for example, 1-Cbz-4-Methylaminopieridine(cas: 405057-75-2Reference of 1-Cbz-4-Methylaminopieridine)

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Reference of 1-Cbz-4-Methylaminopieridine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Blizzard, Timothy A.’s team published research in Bioorganic & Medicinal Chemistry Letters in 2014 | CAS: 405057-75-2

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Recommanded Product: 1-Cbz-4-Methylaminopieridine

Blizzard, Timothy A.; Chen, Helen; Kim, Seongkon; Wu, Jane; Bodner, Rena; Gude, Candido; Imbriglio, Jason; Young, Katherine; Park, Young-Whan; Ogawa, Aimie; Raghoobar, Susan; Hairston, Nichelle; Painter, Ronald E.; Wisniewski, Doug; Scapin, Giovanna; Fitzgerald, Paula; Sharma, Nandini; Lu, Jun; Ha, Sookhee; Hermes, Jeff; Hammond, Milton L. published an article on February 1 ,2014. The article was titled 《Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Recommanded Product: 1-Cbz-4-Methylaminopieridine The information in the text is summarized as follows:

β-Lactamase inhibitors with a bicyclic urea core and a variety of heterocyclic side chains were prepared and evaluated as potential partners for combination with imipenem to overcome class A and C β-lactamase mediated antibiotic resistance. The piperidine analog 3 (MK-7655) inhibited both class A and C β-lactamases in vitro. It effectively restored imipenem’s activity against imipenem-resistant Pseudomonas and Klebsiella strains at clin. achievable concentrations A combination of MK-7655 and Primaxin is currently in phase II clin. trials for the treatment of Gram-neg. bacterial infections. In the experiment, the researchers used many compounds, for example, 1-Cbz-4-Methylaminopieridine(cas: 405057-75-2Recommanded Product: 1-Cbz-4-Methylaminopieridine)

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Recommanded Product: 1-Cbz-4-Methylaminopieridine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

The important role of 405057-75-2

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 405057-75-2, and how the biochemistry of the body works.Application of 405057-75-2

Application of 405057-75-2, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.405057-75-2, Name is 1-Cbz-4-Methylaminopieridine, molecular formula is C14H20N2O2. In a article，once mentioned of 405057-75-2

Inhibition of kinesin spindle protein (KSP) is a novel mechanism for treatment of cancer with the potential to overcome limitations associated with currently employed cytotoxic agents. Herein, we describe a C2-hydroxymethyl dihydropyrrole KSP inhibitor (11) that circumvents hERG channel binding and poor in vivo potency, issues that limited earlier compounds from our program. However, introduction of the C2-hydroxymethyl group caused 11 to be a substrate for cellular efflux by P-glycoprotein (Pgp). Utilizing knowledge garnered from previous KSP inhibitors, we found that beta-fluorination modulated the pK a of the piperidine nitrogen and reduced Pgp efflux, but the resulting compound (14) generated a toxic metabolite in vivo. Incorporation of fluorine in a strategic, metabolically benign position by synthesis of an N-methyl-3-fluoro-4-(aminomethyl)piperidine urea led to compound 30 that has an optimal in vitro and metabolic profile. Compound 30 (MK-0731) was recently studied in a phase I clinical trial in patients with taxane-refractory solid tumors.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 405057-75-2, and how the biochemistry of the body works.Application of 405057-75-2

Reference：
Piperidine – Wikipedia,
Piperidine | C5H20713N – PubChem