80241-82-3Relevant academic research and scientific papers
Highly enantioselective synthesis of 2,3-dihydro-1 H-imidazo[2,1-a isoindol-5(9b H)-ones via catalytic asymmetric intramolecular cascade imidization-nucleophilic addition-lactamization
He, Yuwei,Cheng, Chuyu,Chen, Bin,Duan, Kun,Zhuang, Yue,Yuan, Bo,Zhang, Meisan,Zhou, Yougui,Zhou, Zihong,Su, Yu-Jun,Cao, Rihui,Qiu, Liqin
, p. 6366 - 6369 (2015/01/16)
Highly enantioselective catalytic asymmetric intramolecular cascade imidization-nucleophilic addition-lactamization of N1-alkylethane-1,2-diamine with methyl 2-formylbenzoate catalyzed by a chiral phosphoric acid represents the first efficient method for the preparation of medicinally interesting chiral 2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-ones with high yields and excellent enantioselectivities. This strategy has been shown to be quite general toward various methyl 2-formylbenzoates.
PYRIDINYL AND FUSED PYRIDINYL TRIAZOLONE DERIVATIVES
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Paragraph 0255-0256, (2014/09/29)
Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.
Probing the reactivity of o-phthalaldehydic acid/methyl ester: Synthesis of N-isoindolinones and 3-arylaminophthalides
Mamidyala, Sreeman K.,Cooper, Matthew A.
supporting information, p. 8407 - 8409 (2013/09/23)
A new method for the synthesis of N-substituted isoindolinones and 3-arylaminophthalides was developed through aza-Wittig/cyclisation. The reaction of o-phthalaldehydic acid methyl ester with benzylic, aromatic and aliphatic azides gave N-isoindolinones w
Efficient synthesis of anacardic acid analogues and their antibacterial activities
Mamidyala, Sreeman K.,Ramu, Soumya,Huang, Johnny X.,Robertson, Avril A.B.,Cooper, Matthew A.
, p. 1667 - 1670 (2013/04/10)
Anacardic acid derivatives exhibit a broad range of biological activities. In this report, an efficient method for the synthesis of anacardic acid derivatives was explored, and a small set of salicylic acid variants synthesised retaining a constant hydrophobic element (a naphthyl tail). The naphthyl side chain was introduced via Wittig reaction and the aldehyde installed using directed ortho-metalation reaction of the substituted o-anisic acids. The failure of ortho-metalation using unprotected carboxylic acid group compelled us to use directed ortho-metalation in which a tertiary amide was used as a strong ortho-directing group. In the initial route, tertiary amide cleavage during final step was challenging, but cleaving the tertiary amide before Wittig reaction was beneficial. The Wittig reaction with protected carboxylic group (methyl ester) resulted in side-products whereas using sodium salt resulted in higher yields. The novel compounds were screened for antibacterial activity and cytotoxicity. Although substitution on the salicylic head group enhanced antibacterial activities they also enhanced cytotoxicity.
A conventional approach to the total synthesis of (-)-varitriol
Vamshikrishna,Srihari
, p. 1584 - 1587 (2013/02/22)
The stereoselective total synthesis of (-)-varitriol has been achieved starting from commercially available d-(-)-ribose and o-anisic acid. A Mitsunobu reaction, Julia-Kocienski olefination, and one pot reduction of both ester and iodo functionalities with superhydride are the key reactions involved in this synthesis.
DBU-CH3I, a potential substitute for CH2N2 in the preparation of methyl esters and methyl aryl ethers: Studies with assorted acids
Mal, Dipakranjan,Jana, Amit,Ray, Sutapa,Bhattacharya, Sourav,Patra, Asit,De, Saroj R.
experimental part, p. 3937 - 3946 (2009/04/11)
DBU-CH3I has been poised to be a substitute for diazomethane in the preparation of methyl esters from carboxylic acids. The reactions can be carried out in commercial untreated acetone and acetonitrile, which have been exemplified with several methyl esters, otherwise it is difficult to prepare. Bis-esterification using diiodomethane can also be achieved in a similar fashion. Sufficiently acidic phenols are also conveniently O-methylated by the method. Copyright Taylor & Francis Group, LLC.
Photochemical Transformations of Methoxyphthalaldehydic Esters: Synthesis of Methyl 6-Methoxyphthalaldehydate from the 3-Methoxy-isomer
Jung, Michael E.,Blum, Roberto B.
, p. 962 - 963 (2007/10/02)
Irradiation of the 3-methoxyphthalaldehydate (4a) in methanol gives an excellent yield of the methoxyphthalide (1c) which can be converted into the 6-methoxyphthalaldehydate (3a) in excellent yield, thus effecting an 'isomerization' of the original phthal
