Category: 1172500-91-2

Chang, Edcon et al. published their patent in 2009 |CAS: 1172500-91-2

The Article related to pyrazolopyrimidine preparation apoptosis signal regulating kinase 1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: piperidines

On October 8, 2009, Chang, Edcon; Duong, Tracy; Hirano, Takehiro; Mcneill, Matthew H.; Terao, Yoshito; Vassar, Angie published a patent.Category: piperidines The title of the patent was Preparation of pyrazolo[1,5-a]pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors. And the patent contained the following:

The invention is related to the preparation of pyrazolo[1,5-a]pyrimidines I [R1 = H, OH, (un)substituted aryloxy, sulfonylalkyl, heteroaryl, etc.; R2 = NO2, CN, (un)substituted haloalkyl, heterobicycloalkyl, aryl, etc.; provided that R2 is not an unsubstituted n-(C1-3)alkyl; R3 = H, halo, NH2, (un)substituted azaalkyl, heteroarylalkyl, etc.] and their pharmaceutically acceptable salts as inhibitors of apoptosis signal-regulating kinase 1 (ASK1) and to their pharmaceutical compositions containing them. Thus, cyclization of 5-methyl-1H-pyrazol-3-amine with Et 3-ethoxy-3-iminopropionate hydrochloride, treatment of 5-amino-2-methylpyrazolo[1,5-a]pyrimidin-7(4H)-one with POCl3 at 95-105°, conversion of phosphorylated intermediate (no data) to 7-chloro-2-methylpyrazolo[1,5-a]pyrimidin-5-amine, acylation of the amine with 4-tert-butylbenzoyl chloride and Pd-coupling of the chloride with [3-(hydroxymethyl)phenyl]boronic acid gave pyrazolopyrimidine II. The enzyme activity of selected I against ASK1 was determined in a scintillation assay. The experimental process involved the reaction of 4-Benzenesulfonylpiperidine Hydrochloride(cas: 1172500-91-2).Category: piperidines

The Article related to pyrazolopyrimidine preparation apoptosis signal regulating kinase 1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Accetta, Alessandro et al. published their patent in 2020 |CAS: 1172500-91-2

The Article related to human, asthma chronic obstructive pulmonary idiopathic fibrosis hypertension, rho kinase inhibitor tyrosine amide amino acid preparation copd, tyrosine amide rho kinase inhibitor preparation rock1 rock2 pulmonary and other aspects.Name: 4-Benzenesulfonylpiperidine Hydrochloride

On January 23, 2020, Accetta, Alessandro; Rancati, Fabio; Capelli, Anna Maria; Clark, David Edward; Tisselli, Patrizia; Edwards, Christine; Cheguillaume, Arnaud Jean Francois Auguste; Bhalay, Gurdip published a patent.Name: 4-Benzenesulfonylpiperidine Hydrochloride The title of the patent was Preparation of tyrosine amide derivatives as Rho-kinase inhibitors. And the patent contained the following:

The invention relates to compounds of formula I and pharmaceutically acceptable salts and solvates thereof, wherein X1 and X2 are independently CH and N; p = 1 – 3; each R when present is halo; R0 and R1 are independently H, halo, CN, etc.; R2 and R3 are independently H, C1-6 alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl; R4 and R5 are independently H, C1-6 alkyl;R6 is H, alkyl, haloalkyl; were prepared and used as Rho kinase inhibitors. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). Example compound II was prepared. The invention compounds were evaluated for their Rho-associated protein kinase ROCK1 and ROCK2 inhibitory activities. From the assay, it was determined that compound II exhibited Ki value of < 3 nM. The experimental process involved the reaction of 4-Benzenesulfonylpiperidine Hydrochloride(cas: 1172500-91-2).Name: 4-Benzenesulfonylpiperidine Hydrochloride

The Article related to human, asthma chronic obstructive pulmonary idiopathic fibrosis hypertension, rho kinase inhibitor tyrosine amide amino acid preparation copd, tyrosine amide rho kinase inhibitor preparation rock1 rock2 pulmonary and other aspects.Name: 4-Benzenesulfonylpiperidine Hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Brief introduction of 1172500-91-2

As the paragraph descriping shows that 1172500-91-2 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1172500-91-2,4-Benzenesulfonylpiperidine Hydrochloride,as a common compound, the synthetic route is as follows.

A solution of JV-(7-chloro-2-methylpyrazolo[l ,5-alpha]pyrimidin-5-yl)-4-(2- hydroxypropan-2-yl)benzamide (2F, 86 mg, 0.25 mmol), 4-(phenylsulfonyl)piperidine hydrochloride (145 mg, 0.50 mmol), and JV,jV-diisopropylethylamine (116 mg, 0.90 mmol) in DMF (1.0 mL) was stirred at 100 0C for 2h. After cooling to room temperature, the mixture was diluted with a few drops of DMSO and methanol, and was then purified by preparatory HPLC (40-55% MeCN/H2O gradient + 0.01% TFA). Lyophilization of the combined fractions gave the titled compound as a white solid (97.2 mg, 73%). 1H NMR (DMSO-d6) delta: 10.90 (s, IH), 7.99 (d, J = 8.8 Hz, 2H), 7.89 – 7.95 (m, 2H), 7.78 – 7.85 (m, IH), 7.68 – 7.76 (m, 2H), 7.60 (d, 2H), 7.28 (s, IH), 6.18 (s, IH), 4.53 (d, J = 12.6 Hz, 2H), 3.69 (tt, J = 11.8, 3.7 Hz, IH), 3.00 – 3.11 (m, 2H), 2.37 (s, 3H), 2.04 (d, J = 10.9 Hz, 2H), 1.75 (qd, J = 12.3, 3.8 Hz, 2H), 1.45 (s, 6H); ESI-MS: m/z 534.2 (M+H)+., 1172500-91-2

As the paragraph descriping shows that 1172500-91-2 is playing an increasingly important role.

Reference：
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; WO2009/123986; (2009); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem

 

Some tips on 1172500-91-2

1172500-91-2, The synthetic route of 1172500-91-2 has been constantly updated, and we look forward to future research findings.

1172500-91-2, 4-Benzenesulfonylpiperidine Hydrochloride is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 4-(phenylsulfonyl)piperidine hydrochloride (l .Og, 3.8 mmol), (S)-2-((tert-butoxycarbonyl)amino)-3-(3,5-difluoro-4-hydroxyphenyl)propanoic acid (l .lg, 3.5 mmol), DIPEA (1.8 mL, 10.4 mmol), DCM (16 mL) and DMF (4 mL) was treated with HATU (1.59 g, 4.2 mmol). The mixture was stirred for lh then the resulting solution was allowed to stand for 18 h. The mixture was diluted with dichloro methane (30 mL) and washed with saturated sodium hydrogen carbonate (aq.) (20 mL) then saturated brine (2 x 20 mL). The organic phase was dried (Na2S04) and concentrated in vacuo and purified by chromatography on a Si cartridge eluting with 0-20% DCM in ethyl acetate to give Intermediate 41 A (780 mg). LCMS (Method 3): Rt = 1.25 min. m/z 525.3 [M+H]+

1172500-91-2, The synthetic route of 1172500-91-2 has been constantly updated, and we look forward to future research findings.

Reference：
Patent; CHIESI FARMACEUTICI S.P.A.; ACCETTA, Alessandro; RANCATI, Fabio; CAPELLI, Anna Maria; CLARK, David Edward; TISSELLI, Patrizia; EDWARDS, Christine; CHEGUILLAUME, Arnaud Jean Francois Auguste; BHALAY, Gurdip; (101 pag.)WO2020/16129; (2020); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem