105250-17-7Relevant academic research and scientific papers
Preparation method of 2-aminopyridine-4-methyl alcohol intermediate
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Paragraph 0025; 0032; 0039; 0046; 0053, (2019/01/23)
The invention discloses a preparation method of a 2-aminopyridine-4-methyl alcohol intermediate. The preparation method includes the following steps of adopting 4-methylpyridine-2-formaldehyde as a raw material and making the raw material subjected to a chlorine substitute reaction to convert methyl into chloromethyl; then conducting an oxidizing reaction to convert formyl into carboxyl; then making the raw material react with triethylamine and DPPA to convert carboxyl into amino and oxidizing chloromethyl into hydroxymethyl to obtain 2-aminopyridine-4-methyl alcohol. The preparation method issimple in operation, mild in condition and high in product purity and product yield and generates few by-products.
Spin-Center Shift-Enabled Direct Enantioselective α-Benzylation of Aldehydes with Alcohols
Nacsa, Eric D.,MacMillan, David W. C.
supporting information, p. 3322 - 3330 (2018/03/13)
Nature routinely engages alcohols as leaving groups, as DNA biosynthesis relies on the removal of water from ribonucleoside diphosphates by a radical-mediated "spin-center shift" (SCS) mechanism. Alcohols, however, remain underused as alkylating agents in synthetic chemistry due to their low reactivity in two-electron pathways. We report herein an enantioselective α-benzylation of aldehydes using alcohols as alkylating agents based on the mechanistic principle of spin-center shift. This strategy harnesses the dual activation modes of photoredox and organocatalysis, engaging the alcohol by SCS and capturing the resulting benzylic radical with a catalytically generated enamine. Mechanistic studies provide evidence for SCS as a key elementary step, identify the origins of competing reactions, and enable improvements in chemoselectivity by rational photocatalyst design.
Method for synthesizing 2-aminopyridine-4-methanol
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Paragraph 0022-0053, (2018/04/21)
The invention discloses a method for synthesizing 2-aminopyridine-4-methanol. The method comprises the following steps that 4-pyridylcarbinol reacts with an aqueous formamide solution to prepare a second compound; the second compound and a NaOH solution are mixed and placed into a reaction still, the temperature is controlled within 5-10 DEG C, a NaBrO solution is added dropwise into the reactionstill, after the dropwise addition is completed, the reaction is continuously conducted for 1-2 hours at the temperature, then the temperature is raised to 50-60 DEG C to enable the reaction to be conducted continuously for 1 hour and then reduced to room temperature, ethyl acetate is used for carrying out extraction several times, organic phases are combined, distillation under reduced pressure is conducted to remove ethyl acetate, and 2-aminopyridine-4-methanol is prepared. The synthesis method has the advantages that the operation is simple, the conditions are mild, few byproducts are generated, and the product purity and yield are high.
Preparation method of 2-aminopyridine-4-methanol medical intermediate
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, (2017/01/12)
The invention discloses a preparation method of a 2-aminopyridine-4-methanol medical intermediate. By virtue of the preparation method, the 2-aminopyridine-4-methanol medical intermediate is prepared from 2-aminopyridine-4-methyl sequentially through acet
NOVEL COMPOUND, ORGANIC CATION TRANSPORTER 3 DETECTION AGENT, AND ORGANIC CATION TRANSPORTER 3 ACTIVITY INHIBITOR
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Paragraph 0515-0516; 0519-0520, (2016/08/17)
[Problem] The present invention addresses the problem of providing a novel compound. The present invention also addresses the problem of providing an OCT3 detection agent or an OCT3 activity inhibitor, which comprises the novel compound. [Solution] A compound represented by formula (A), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. ????????R1-R2-R3-R4?????(A)
SELECTIVE INHIBITORS AGAINST Cdk4 AND Cdk6 HAVING AMINOTHIAZOLE SKELETON
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Page/Page column 77, (2010/11/25)
The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH 2 ; Y 1 , Y 2 , Y 3 , Y 4 and Y 5 , which may be identical or different, are each CH or N; however, at least one of Y 1 , Y 2 , Y 3 , Y 4 and Y 5 is N; Z 1 and Z 2 , which may be identical or different, are each CH or N; n is an integer from 1 to 3; R 1 is a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R 2 and R 3 , which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, an aromatic heterocyclic ring, or the like; and R 4 is a hydrogen atom, a lower alkyl group, a C 3 -C 6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.
NOVEL C3A RECEPTOR ANTAGONISTS
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Page/Page column 58, (2010/11/26)
Aryl substituted imidazo[4,5-c] pyridine compounds are provided. These compounds are useful in pharmaceutical compositions as C3a antagonists for treating a variety of medical conditions associated with the Complement cascade. Methods for treating such conditions are also provided.
PIPERIDINE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS
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Page/Page column 51, (2010/11/25)
Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)
Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents
Feng, Dennis,Fisher, Michael,Liang, Gui-Bai,Qian, Xiaoxia,Brown, Chris,Gurnett, Anne,Leavitt, Penny Sue,Liberator, Paul A.,Mathew, John,Misura, Andrew,Samaras, Samantha,Tamas, Tamas,Schmatz, Dennis M.,Wyvratt, Matthew,Biftu, Tesfaye
, p. 5978 - 5981 (2007/10/03)
Compounds 10a-10d and 10i are very potent inhibitors of Eimeria tenella cGMP-dependent protein kinase (0.081-0.32 nM) and are very efficacious antiparasitic agents in vivo when administered to chickens at 12.5-25 ppm levels in the feed.
