Day: October 28, 2022

On October 7, 1982, Sazonov, N. V.; Grineva, N. A.; Safonova, T. S. published a patent.Safety of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine The title of the patent was Pyrimido[4,5-b][1,4]benzoxazepine derivatives. And the patent contained the following:

I (R = Cl, OH, NH2, benzyl- or phenyl-substituted amino, N-methylpiperazino, R1 = H; R = butyl- or benzyl-substituted amino, morpholino, piperidino, R1 = Br; R = morpholino, R1 = NO2) were prepared by treating aminochloropyrimidines II with hydroxybenzaldehydes III (or alk. salts) in DMF or toluene at 100-20°. The experimental process involved the reaction of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine(cas: 84762-70-9).Safety of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine

The Article related to pyrimidobenzoxazepine amino, benzoxazepine pyrimido, oxazepine pyrimidobenz, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Safety of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 31, 1985, Levkovskaya, L. G.; Sazonov, N. V.; Grineva, N. A.; Mamaeva, I. E.; Serochkina, L. A.; Safonova, T. S. published an article.COA of Formula: C9H13ClN4 The title of the article was Study of nitrogen- and oxygen-containing heterocycles. 42. Pyrimido[4,5-b]- and pyrido[2,3-b]-1,4-benzoxazepines. And the article contained the following:

Oxazepines I (R = H, Cl, R1X = N, CH, ClCH, R2 = NHCH2Ph, NHPh, piperidino, morpholino, NH2, Cl, OH, 1-methylpiperazinyl, H) were prepared in 25-95% yields by cyclocondensation of pyridines or pyrimidines II wiwth 5,2-R3YC6H3CHO in DMF containing NaH. Reduction of I by NaBH4 in absolute EtOH gave 76-100% of the corresponding 5,6-dihydro derivatives The experimental process involved the reaction of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine(cas: 84762-70-9).COA of Formula: C9H13ClN4

The Article related to benzopyridooxazepine, benzopyrimidooxazepine, pyridooxazepine benzo, pyrimidooxazepine, oxazepine pyrido pyrimido, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.COA of Formula: C9H13ClN4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhu, Xue Y.; Etukala, Jagan R.; Eyunni, Suresh V. K.; Setola, Vincent; Roth, Bryan L.; Ablordeppey, Seth Y. published an article in 2012, the title of the article was Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): A search for new dual-acting agents as potential antidepressants.HPLC of Formula: 39512-49-7 And the article contains the following content:

The synthesis and evaluation of several benzothiazole-based compounds are described in an attempt to identify novel dual-acting 5HT1A receptor and SERT inhibitors as new antidepressants. Binding affinities at the 5HT1A receptor and the serotonin transporter do not appear to be congruent and other areas of the binding sites would need to be explored in order to improve binding simultaneously at both sites. Compounds I and II show moderate binding affinity at the 5HT1A receptor and the SERT site and thus, have the potential to be further explored as dual-acting agents. In addition, compound I binds with low affinity to the dopamine transporter (DAT), the norepinephrine transporter (NET) and 5HT2C receptor, which are desirable properties as selectivity for SERT (and not DAT or NET) is associated with an absence of cardiovascular side effects. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).HPLC of Formula: 39512-49-7

The Article related to benzothiazole preparation 5ht1a receptor sert inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Klochkov, S. G.; Anan’ev, I. V.; Pukhov, S. A.; Afanas’eva, S. V. published an article in 2012, the title of the article was Stereochemistry of the aza-Michael reaction with natural alantolactones.Related Products of 39512-49-7 And the article contains the following content:

Hydrogenated 3-aminomethylnaphtho[2,3-b]furan-2-ones were synthesized by the reaction of natural alantolactones with pharmacophoric amines. Determination of the newly formed asym. center configuration by two-dimensional NMR data is presented. The structure of the obtained compounds was proved by X-ray structural anal. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Related Products of 39512-49-7

The Article related to stereochem aza michael reaction natural alantolactone, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Related Products of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Cabrero-Antonino, Jose R.; Leyva-Perez, Antonio; Corma, Avelino published an article in 2012, the title of the article was Regioselective Hydration of Alkynes by Iron(III) Lewis/Bronsted Catalysis.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

The triflimide iron(III) salt [Fe(NTf2)3] promotes the direct hydration of terminal and internal alkynes with very good Markovnikov regioselectivities and high yields. The enhanced carbophilic Lewis acidity of the FeIII cation mediated by the weakly-coordinating triflimide anion is crucial for the catalytic activity. The iron(III) metal salt can be recycled as the OPPh3/[Fe(NTf2)3] system with similar activity and selectivity. However, spectroscopic and kinetic studies show that [Fe(NTf2)3] hydrolyzes under the reaction conditions and that catalytically less active Broensted species are formed, which points to a Lewis/Broensted co-catalysis. This triflimide-based catalytic system is regioselective for the hydration of internal aryl-alkynes and opens the door to a new synthetic route to alkyl ketophenones. As a proof of concept, the synthesis of two antipsychotics Haloperidol and Melperone, with general butyrophenone-like structure, is shown. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to regioselective hydration alkyne iron lewis broensted catalysis, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On April 23, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Safety of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate The title of the patent was Preparation of 4-aminopyrimidines as CGRP antagonists. And the patent contained the following:

Title compounds I [R1 = spirocylic heterocycles with provisos; R2 = H, alkyl, etc.; R3 = aryl, heteroaryl, etc.; U = N, N-oxide, etc.; V = N, N-oxide, etc.; X = N, N-oxide, etc.; Y = N, C-R7; R7 = H, halo, alkyl] and their pharmaceutically acceptable salts and formulations were prepared For example, N-arylation of a piperidine II and chloropyrimidine III afforded claimedaminopyrimidine IV in 55% yield. In CGRP inhibition assays, 2-examples of compounds I exhibited Ki values of 6 and 27 nM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Safety of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

The Article related to aminopyrimidine preparation cgrp antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 28, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Synthetic Route of 883984-95-0 The title of the patent was Preparation of as 2-oxoindoles CGRP receptor antagonists. And the patent contained the following:

Title compounds I [R1 = 2-oxoindole with provisos; R2 = H, alkyl; R3 = H, alkylene, etc.; R4 = H, alkylene, etc.; U = N, N-oxide, CR5; V = N, N-oxide, CR6; X = N, N-oxide, CR7; Y = N, CR6; R5 = H, hyalo, CN, etc.; R6 = H, alkyl, etc.; R7 = H, halo, CN. etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, coupling of chloropyrimide II and amine III afforded claimed oxoindole IV. In CGRP receptor antagonists assays, 4-examples of compounds I exhibited Ki values ranging from 15-535 nM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Synthetic Route of 883984-95-0

The Article related to oxoindole preparation cgrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 28, 2009, Gottschling, Dirk; Dahmann, Georg; Doods, Henri; Heimann, Annekatrin; Mueller, Stephan Georg; Rudolf, Klaus; Schaenzle, Gerhard; Stenkamp, Dirk published a patent.Synthetic Route of 883984-95-0 The title of the patent was Preparation of as pyridin-2-ones as CGRP receptor antagonists. And the patent contained the following:

Title compounds I and II [R1 = 2-oxoindoles with provisos; R2 = H, alkyl; R3 = H, alkylene, etc.; R4 = H, alkylenen, etc.; R5 = H, alkyl, benzyl, etc.;] and their pharmaceutically acceptable salts and formulations were prepared For example, deprotection of methoxypyridine III afforded claimed pyridinone IV. In CGRP receptor antagonists assays, compounds I and II exhibited Ki values ≤50 μM. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Synthetic Route of 883984-95-0

The Article related to pyridinone preparation cgrp receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 9, 2020, Ji, Nan; Mainolfi, Nello; Weiss, Matthew published a patent.Synthetic Route of 1251006-64-0 The title of the patent was Preparation of novel bifunctional compounds as MerTK degraders and uses thereof. And the patent contained the following:

The present invention provides compounds I [TAMBM is an TAM receptor kinase binding moiety; L is a bivalent moiety that connects TAMBM to DIM; and DIM is a degradation inducing moiety selected from LBM, a lysine mimetic, and H] or pharmaceutically acceptable salts thereof, compositions thereof, and methods of using the same. E.g., a multi-step synthesis of trans-II, starting from Et 4-chloro-2-(methylsulfanyl)pyrimidine-5-carboxylate, was described. Exemplified compounds I were tested for MerTK degradation in vitro (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Synthetic Route of 1251006-64-0

The Article related to bifunctional compound preparation mertk degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 1251006-64-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 24, 2022, Xu, Junyu; Li, Youbin; Zheng, Danyang; Wang, Xuesong; Wang, Yan; Tan, Yinfeng; Wang, Yong; Yang, Chenqi; Zhang, Yuchen; Guo, Tong published a patent.Related Products of 1216805-11-6 The title of the patent was Preparation method of N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)formamide derivative, and application thereof in preparation of drugs for treating and/or preventing hyperproliferative diseases. And the patent contained the following:

The title N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)formamide derivative is obtained by covalently linking T or Q and T with N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)formamide fragment, and has structural formulas as shown in claim 1, wherein Q is linking group, and is linear or branched alkylene chain composed of 1-10 CH2 or CH, and the linear or branched alkylene chain is linked with T via -NH-; and T is any one of fragments having structural formulas as shown in claim 1. The derivative has a specific structural formula as shown in claim 2, and is 2-(2,6-dioxopiperidin-3-yl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-1,3-dioxoisoindoline-5-carboxamide. The derivative can effectively inhibit activity of human chronic myeloid leukemia cells and human gastrointestinal stromal tumor cells, and can be used in the preparation of drugs for treatment and/or prevention of hyperproliferative diseases, in particular for treatment of chronic myeloid leukemia and gastrointestinal stromal tumor. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Related Products of 1216805-11-6

The Article related to formamide pyrimidinylaminophenyl preparation hyperproliferative disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem