Category: 120014-30-4

Direct Catalytic Decarboxylative Amination of Aryl Acetic Acids was written by Kong, Duanyang;Moon, Patrick J.;Bsharat, Odey;Lundgren, Rylan J.. And the article was included in Angewandte Chemie, International Edition in 2020.Related Products of 120014-30-4 This article mentions the following:

The decarboxylative coupling of a carboxylic acid with an amine nucleophile provides an alternative to the substitution of traditional organohalide coupling partners. Benzoic and alkynyl acids may be directly aminated by oxidative catalysis. In contrast, methods for intermol. alkyl carboxylic acid to amine conversion, including amidate rearrangements and photoredox-promoted approaches, require stoichiometric activation of the acid unit to generate isocyanate or radical intermediates. Reported here is a process for the direct chemoselective decarboxylative amination of electron-poor arylacetates by oxidative Cu catalysis. The reaction proceeds at (or near) room temperature, uses native carboxylic acid starting materials, and is compatible with protic, electrophilic, and other potentially complicating functionality. Mechanistic studies support a pathway in which ionic decarboxylation of the acid generates a benzylic nucleophile which is aminated in a Chan-Evans-Lam-type process. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4Related Products of 120014-30-4).

5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Related Products of 120014-30-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

1-Benzyl-4-methylpiperidinyl moiety in donepezil: The priority ticket across the blood-brain-barrier in rats was written by Zdarova Karasova, Jana;Sestak, Vit;Korabecny, Jan;Mezeiova, Eva;Palicka, Vladimir;Kuca, Kamil;Mzik, Martin. And the article was included in Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences in 2018.Electric Literature of C17H23NO3 This article mentions the following:

The main aim of the authors’ study was to clarify which part of the donepezil mol. determines its ability to cross the blood-brain barrier (BBB). The authors developed and fully validated a rapid, selective and sensitive method to quantify donepezil and its three fragments in rat plasma and brain homogenate, employing ultra-HPLC with high resolution mass spectrometry (Orbitrap, Q-Exactive Focus), and used it to assess the pharmacokinetics after concomitant administration of donepezil and its three fragments. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4Electric Literature of C17H23NO3).

5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Electric Literature of C17H23NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis of Donepezil Hydrochloride via Chemoselective Hydrogenation was written by Rawat, Ajay Singh;Pande, Sachin;Bhatt, Nilay;Kharatkar, Raju;Belwal, Chandrakant;Vardhan, Anand. And the article was included in Organic Process Research & Development in 2013.Recommanded Product: 120014-30-4 This article mentions the following:

A simple and highly chemoselective and cost-effective process for the synthesis of Donepezil 1 has been developed for com. production In the process, the exocyclic double bond is mainly targeted for catalytic hydrogenation in the presence of an N-benzyl group using sulfur, nitrogen, and phosphorous catalyst modifiers. In some cases, catalytic hydrogenation with Pd on charcoal also produced an undesired side product along with the main product due to over reduction Removal of these impurities by crystallization, column chromatog., or other means of purification makes the process tedious and lengthy, and sometimes it is difficult to achieve the impurity limit as per International Conference on Harmonisation (ICH) guidelines for active pharmaceutical ingredients. In the present investigation we report the synthesis of Donepezil 1 in pure form wherein the debenzyl impurity is within the acceptable limits. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4Recommanded Product: 120014-30-4).

5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 120014-30-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

New gradient high-performance liquid chromatography method for determination of donepezil hydrochloride assay and impurities content in oral pharmaceutical formulation was written by Kafkala, Stella;Matthaiou, Stella;Alexaki, Pandora;Abatzis, Morfis;Bartzeliotis, Antonios;Katsiabani, Maria. And the article was included in Journal of Chromatography A in 2008.HPLC of Formula: 120014-30-4 This article mentions the following:

A new gradient HPLC method has been developed and validated for the determination of both assay and related substances of donepezil hydrochloride in oral pharmaceutical formulation. Different kinds of columns and gradient elution programs were tested in order to achieve satisfactory separation between the active substance, 4 impurities and an interfering excipient used in the formulation. Best results were obtained using an Uptisphere ODB C₁₈ column 250 mm 脳 4.6 mm, 5 渭m, UV detection at 270 nm and a gradient elution of phosphate buffer (0.005M, pH 3.67) and methanol as the mobile phase. The method was validated with respect to linearity, precision, accuracy, specificity and robustness. It was also a stability-indicating method, and therefore suitable for the routine anal. of donepezil and related substances in the pharmaceutical formulation. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4HPLC of Formula: 120014-30-4).

5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.HPLC of Formula: 120014-30-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A photochemical dehydrogenative strategy for aniline synthesis was written by U. Dighe, Shashikant;Julia, Fabio;Luridiana, Alberto;Douglas, James J.;Leonori, Daniele. And the article was included in Nature (London, United Kingdom) in 2020.Application In Synthesis of 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one This article mentions the following:

Chem. reactions that reliably join two mol. fragments together (cross-couplings) are essential to the discovery and manufacture of pharmaceuticals and agrochems.^1,2. The introduction of amines onto functionalized aromatics at specific and pre-determined positions (ortho vs. meta vs. para) is currently achievable only in transition-metal-catalyzed processes and requires halogen- or boron-containing substrates^3-6. The introduction of these groups around the aromatic unit is dictated by the intrinsic reactivity profile of the method (electrophilic halogenation or C-H borylation) so selective targeting of all positions is often not possible. Here we report a non-canonical cross-coupling approach for the construction of anilines, exploiting saturated cyclohexanones as aryl electrophile surrogates. Condensation between amines and carbonyls, a process that frequently occurs in nature and is often used by (bio-)organic chemists⁷, enables a predetermined and site-selective carbon-nitrogen (C-N) bond formation, while a photoredox- and cobalt-based catalytic system progressively desaturates the cyclohexene ring en route to the aniline. Given that functionalized cyclohexanones are readily accessible with complete regiocontrol using the well established carbonyl reactivity, this approach bypasses some of the frequent selectivity issues of aromatic chem. We demonstrate the utility of this C-N coupling protocol by preparing com. medicines and by the late-stage amination-aromatization of natural products, steroids and terpene feedstocks. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4Application In Synthesis of 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one).

5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A photochemical dehydrogenative strategy for aniline synthesis was written by U. Dighe, Shashikant;Julia, Fabio;Luridiana, Alberto;Douglas, James J.;Leonori, Daniele. And the article was included in Nature (London, United Kingdom) in 2020.Application In Synthesis of 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one This article mentions the following:

Chem. reactions that reliably join two mol. fragments together (cross-couplings) are essential to the discovery and manufacture of pharmaceuticals and agrochems.^1,2. The introduction of amines onto functionalized aromatics at specific and pre-determined positions (ortho vs. meta vs. para) is currently achievable only in transition-metal-catalyzed processes and requires halogen- or boron-containing substrates^3-6. The introduction of these groups around the aromatic unit is dictated by the intrinsic reactivity profile of the method (electrophilic halogenation or C-H borylation) so selective targeting of all positions is often not possible. Here we report a non-canonical cross-coupling approach for the construction of anilines, exploiting saturated cyclohexanones as aryl electrophile surrogates. Condensation between amines and carbonyls, a process that frequently occurs in nature and is often used by (bio-)organic chemists⁷, enables a predetermined and site-selective carbon-nitrogen (C-N) bond formation, while a photoredox- and cobalt-based catalytic system progressively desaturates the cyclohexene ring en route to the aniline. Given that functionalized cyclohexanones are readily accessible with complete regiocontrol using the well established carbonyl reactivity, this approach bypasses some of the frequent selectivity issues of aromatic chem. We demonstrate the utility of this C-N coupling protocol by preparing com. medicines and by the late-stage amination-aromatization of natural products, steroids and terpene feedstocks. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4Application In Synthesis of 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one).

5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem