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Systematic Studies of Functional Group Tolerance and Chemoselectivity in Carbene-Mediated Intramolecular Cyclopropanation and Intermolecular C-H Functionalization
Chem Pharm Bull (Tokyo). 2024;72(3):313-318. doi: 10.1248/cpb.c24-00022.ABSTRACTGenerating reliable data on functional group compatibility and chemoselectivity is essential for evaluating the practicality of chemical reactions and predicting retrosynthetic routes. In this context, we performed systematic studies using a functional group evaluation kit including 26 kinds of additives to assess the functional group tolerance of carbene-mediated reactions. Our findings revealed that some intermolecular heteroatom-hydrogen insertion reactions proceed faster than intramolecular cyclopropanation reactions. Lewis basic functional...
Source: Chemical and Pharmaceutical Bulletin - March 18, 2024 Category: Drugs & Pharmacology Authors: Haruki Kanda Ayaka Okabe Shingo Harada Tetsuhiro Nemoto Source Type: research

Organocatalyzed Amine-Free O-Phosphorylation of Alcohols with 4-Methylpyridine N-Oxide
Chem Pharm Bull (Tokyo). 2024;72(3):303-308. doi: 10.1248/cpb.c24-00029.ABSTRACTAmine-free phosphorylation of various alcohols was developed with 4-methylpyridine N-oxide in the presence of 4 Å molecular sieves at room temperature. This mild method gave various phosphorylated products in high yield and could be applied to acid- or base-sensitive substrates. Furthermore, this method was also effective for the chemoselective phosphorylation of diols or polyols.PMID:38479853 | DOI:10.1248/cpb.c24-00029 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - March 13, 2024 Category: Drugs & Pharmacology Authors: Keisuke Yoshida Wataru Hirano Ryuuki Ota Shinji Kitagaki Source Type: research

Dissolution Profiles of Oral Disintegrating Tablet with Taste Masking Granule Polymer Coating in Biorelevant Bicarbonate Buffer
Chem Pharm Bull (Tokyo). 2024;72(3):298-302. doi: 10.1248/cpb.c23-00783.ABSTRACTThe current study aimed to explore the impact of buffer species on the dissolution behavior of orally disintegrating tablets (ODT) containing a basic polymer and its influence on bioequivalence (BE) prediction. Fexofenadine hydrochloride ODT formulations were used as the model formulations, Allegra® as the reference formulation, and generic formulations A and B as the test formulations. Allegra®, generic A, and generic B are ODT formulations that contain aminoalkyl methacrylate copolymers E (Eudragit® E, EUD-E), a basic polymer commonly used...
Source: Chemical and Pharmaceutical Bulletin - March 13, 2024 Category: Drugs & Pharmacology Authors: Masaki Higashino Kiyohiko Sugano Source Type: research

Evaluating a Retro-Inverso Type Inhibitor of HTLV-1 Protease as a Competitive Inhibitor
Chem Pharm Bull (Tokyo). 2024;72(3):309-310. doi: 10.1248/cpb.c23-00879.ABSTRACTThe inhibition mode of a retro-inverso (RI) inhibitor containing a hydroxyethylamine dipeptide isostere against the human T-cell leukemia virus type-1 (HTLV-1) protease was examined. Enzymatic evaluation of the RI-modified inhibitor containing a D-allo-Ile residue revealed that HTLV-1 was competitively inhibited. IC50 values of the RI-modified inhibitor and pepstatin A, a standard inhibitor of aspartic proteases, were nearly equivalent.PMID:38479891 | DOI:10.1248/cpb.c23-00879 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - March 13, 2024 Category: Drugs & Pharmacology Authors: Chiyuki Awahara Daiki Oku Kazuya Kobayashi Yasunao Hattori Source Type: research

Synthesis of a Cyclic Hexaamide Consisting of a Brominated m-Phenylene Repeating Unit
Chem Pharm Bull (Tokyo). 2024;72(3):294-297. doi: 10.1248/cpb.c24-00023.ABSTRACTAiming to synthesize a cyclic hexaamide, 4-bromo-3-(isobutylamino)benzoic acid was subjected to self-condensation reactions in the presence of either dichlorotriphenylphosphorane in 1,1,2,2-tetrachloroethane or tetrachlorosilane in pyridine. However, instead of the targeted cyclic hexaamide, the cyclic triamide and the cyclic tetraamide were obtained. The cyclic hexaamide was successfully synthesized via the self-condensation of the dimer, which was synthesized in five steps from 4-bromo-3-(isobutylamino)benzoic acid. A thorough screening of th...
Source: Chemical and Pharmaceutical Bulletin - March 10, 2024 Category: Drugs & Pharmacology Authors: Akihiro Yokoyama Ayaka Chino Kenta Rakumitsu Source Type: research