Month: November 2022

Ko, Wooseok published the artcileConstruction of bacterial cells with an active transport system for unnatural amino acids, Application In Synthesis of 2418-95-3, the publication is ACS Synthetic Biology (2019), 8(5), 1195-1203, database is CAplus and MEDLINE.

Engineered organisms with an expanded genetic code have attracted much attention in chem. and synthetic biol. research. In this work, engineered bacterial organisms with enhanced unnatural amino acid (UAA) uptake abilities were developed by screening periplasmic binding protein (PBP) mutants for recognition of UAAs. A FRET-based assay was used to identify a mutant PBP (LBP-AEL) with excellent binding affinity (K_d ≈ 500 nM) to multiple UAAs from 37 mutants. Bacterial cells expressing LBP-AEL showed up to 5-fold enhanced uptake of UAAs, which was determined by genetic incorporation of UAAs into a green fluorescent protein and measuring UAA concentration in cell lysates. To the best of our knowledge, this work is the first report of engineering cellular uptake of UAAs and could provide an impetus for designing advanced unnatural organisms with an expanded genetic code, which function with the efficiency comparable to that of natural organisms. The system would be useful to increase mutant protein yield from lower concentrations of UAAs for industrial and large-scale applications. In addition, the techniques used in this report such as the sensor design and the measurement of UAA concentration in cell lysates could be useful for other biochem. applications.

ACS Synthetic Biology published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Application In Synthesis of 2418-95-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Bose, D. Subhas published the artcileTrocCl mediated efficient synthesis of nitriles from primary amides, SDS of cas: 2447-79-2, the publication is Synthetic Communications (2000), 30(16), 3047-3052, database is CAplus.

To establish a rapid conversion method of primary amides to nitriles, various types of carboxamides were treated with 2,2,2-trichloroethyl chloroformate and Et₃N, as a dehydrating agent to obtain the desired nitriles in 82-95% yields.

Synthetic Communications published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, SDS of cas: 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Jaiswal, Yogesh published the artcileAcid-promoted palladium(II)-catalyzed ortho-halogenation of primary benzamides: En route to halo-arenes, Related Products of amides-buliding-blocks, the publication is Catalysis Communications (2019), 105784pp., database is CAplus.

Bronsted acid-promoted palladium(II)-catalyzed regioselective installation of halogens (Br, Cl, and I) to the aromatic ring of benzamide derivatives to afford the halogenated arenes I [R = H, 4-Me, 5-Cl, etc.; X = Cl, Br, I] was achieved using primary amides. Mild reaction conditions, use of primary amide as a directing group, external additive-free conditions and gram-scale reaction were some appealing features of this protocol.

Catalysis Communications published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Santhosh, Akhil published the artcileRandomized double-blind, placebo-controlled study of topical diclofenac in the prevention of hand-foot syndrome in patients receiving capecitabine (the D-TORCH study), SDS of cas: 169590-42-5, the publication is Trials (2022), 23(1), 420, database is CAplus and MEDLINE.

Abstract: Introduction: Hand-foot syndrome (HFS) is a common cutaneous side effect of capecitabine therapy. Apart from oral cyclooxygenase-2 (COX-2) inhibitor (celecoxib), there are no proven strategies for the prevention of HFS. However, celecoxib is associated with significant cardiotoxicity. To date, no study has evaluated the role of topical COX inhibitor, diclofenac. In this study, we aim to compare topical 1% diclofenac gel with placebo in the prevention of capecitabine-induced HFS. Methods: This is a randomized, placebo-controlled, double-blind, parallel-group superiority trial: the Diclofenac Topical in Reducing Capecitabine induced HFS (D-TORCH) study. A total of 264 patients with breast and gastrointestinal malignancies will be randomly allocated (stratified by sex and type of therapy [monotherapy or combination regimen with capecitabine]) to receive either 1% topical diclofenac or placebo that will be applied over the palmar and dorsal surface of the hands twice daily while taking capecitabine for 12 wk. The patients will be followed up until the end of four cycles. The primary objective of this study is to compare the effect of topical diclofenac with placebo in preventing HFS (incidence of NCI CTCAEv5.0 grade 2 or higher HFS). The secondary objective is to compare the effect of topical diclofenac with placebo on preventing all grades of HFS (incidence of NCI CTCv5.0 all grade HFS), time to develop HFS (from the start of capecitabine), patient-reported outcomes (PROs) (HF-HRQoL questionnaire), adherence with the application (self-reported), capecitabine dose changes (number of patients with dose modifications due to HFS) and safety profile (NCICTCv5.0 all grade HFS) Discussion: The D-TORCH study aims to determine if 1% topical diclofenac reduces the incidence of grade 2 or higher HFS in patients receiving capecitabine. To date, there have been a lot of trials for hand-foot syndrome prevention using agents like pyridoxine, vitamin E, carvedilol, and various polyherbal formulations, but none has been found successful. If the trial meets the primary end point, 1% topical diclofenac will be the new standard of care for HFS prevention. Trial registration: Clin. Trials Registry of India CTRI/2021/01/030592. Prospectively registered on Jan. 19, 2021

Trials published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, SDS of cas: 169590-42-5.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Rastogi, R. R. published the artcileKetene SS-acetals. Part 10. Reaction of α-oxoketene SS-acetals with N-alkylcyanoacetamides: a new general method for substituted and fused 2,7-dialkyl-8-amino-5-cyano-2,7-naphthyridine-1,6(2H,7H)-diones, Formula: C5H8N2O, the publication is Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) (1978), 554-8, database is CAplus.

The reaction of α-oxoketene dithioacetals with NCCH₂CONHR (I; R = Me, Et) in the presence of NaOCHMe₂ gave 25-93% 2,7-naphthyridine derivatives via N-alkylpyridone intermediates. E.g., naphthyridine II was obtained (38%) by reaction of (MeS)₂C:CHCOPh with I (R = Me). (MeS)₂C:CRCN (III; R = Ph, p-ClC₆H₄, CN) gave 46-68% pyridones IV (R = Me, Et, R¹ = Ph, p-ClC₆H₄, CN) under similar conditions, whereas cyclic ketene dithioacetals V (n = 1,2) gave 71-80% fused naphthyridines VI (n = 1, 2, R = Me, Et). Naphthonaphthyridones VII (R = Me, Et; n = 1, R¹ = H, OMe; n = 2, R¹ = H) were obtained in high yield from the reaction of ketene dithioacetals VIII (n = 1, R¹ = H, OMe; n = 2, R = H) with I (R = Me, Et).

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, Formula: C5H8N2O.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Baulina, T. V. published the artcileSynthesis, Molecular, and Crystal Structure of Tris(2-carbamoylmethoxyphenyl)phosphine Oxide, Synthetic Route of 79-07-2, the publication is Russian Journal of General Chemistry (2020), 90(10), 1840-1844, database is CAplus.

New tripodal ligand, tris(2-carbamoylmethoxyphenyl)phosphine oxide (I), has been synthesized via the alkylation of tris(2-hydroxyphenyl)phosphine oxide with chloroacetamide. The ligand structure has been studied by means of IR and NMR (¹H, ³¹P) spectroscopy as well as X-ray diffraction.

Russian Journal of General Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Synthetic Route of 79-07-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Mikhailova, T. A. published the artcilePolarographic study of some nitrogen-containing heterocycles, COA of Formula: C10H14N2O, the publication is Zhurnal Obshchei Khimii (1969), 39(1), 26-30, database is CAplus.

Polarographic halfwave potentials were reported in the pH range of 1.85-11.6 for pyridine, quinoline, acridine, their 4-carboxylic acids, and the amides of these acids with N-CHMeCH2Ph grouping. Also included were data on N-(1-methyl-2-phenylethyl)amides of isonicotinic acid with the following 2,6-ring substituents: H, H; Cl, Cl; MeO, MeO; Et2N, Et2N; Cl, MeO; Cl, Et2N. N,N-diethylisonicotinamide with the following 2,6-substituents were also reported: H, H; Cl, Cl; Cl, MeO; MeO, MeO; Cl, Et2N; Et2N, Et2N. The main center of reaction in these compounds is the C:N link which gives the 1st polarographic wave at any pH value. Introduction of 4-substituents with electron-acceptor properties serves to lower the halfwave potential; introduction of electron donor groups in 2,6-positions raises the halfwave potential. The CO2H and CONHR groups cause a 2nd polarographic wave in neutral medium only. Treating the acyl chloride with Et2NH in C6H6 gave the diethylamides of: isonicotinic acid, b3 133°, n20D 1.5238; 2,6-dichloroiso-nicotinic acid (I), m. 82-4°; 2-chloro-6-methoxy analog, b3 153°; and the 2,6-dimethoxy analog, m. 87-8°. Heating the diethylamide of I with Et2NH at 100° 1 day gave the diethylamide of 2-chloro-6-diethylaminoisonicotinic acid, b4 182-4°; similarly, by heating 26 hrs. at 200°, the 2,6-bis(diethylamino)analog, m. 54-6°, b3 185-7°, was prepared

Zhurnal Obshchei Khimii published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H14N2O, COA of Formula: C10H14N2O.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Leonov, O. N. published the artcileSynthesis and properties of N²-acylated polyfluoroalkanamidines, Formula: C6H10F3NO, the publication is Zhurnal Obshchei Khimii (1992), 62(7), 1592-7, database is CAplus.

Acylating HN:C(CF₃)NR₂ (I; R = Me, Et) with R¹COCl (R¹ = CF₃, CHF₂, C₂F₅) in Et₂O containing Et₃N gave 5 corresponding R¹CON:C(CF₃)NR₂ in 64.1-89.1% yield. Analogous reaction of CF₃COCl with HN:C(CF₃)NHMe (II) gave CF₃CON:C(CF₃)NHMe and CF₃CONHC(CF₃):NMe in 45.2% combined yield, and (CF₃)₂C:CO (III) and II gave 86.4% (CF₃)₂CHCON:C(CF₃)NHMe. I (same R) and HN:C(C₂F₅)NEt₂ added to III to give 64.1-93.4% (CF₃)₂CHCON:CR²NR₂ [R = Me, Et (IV), R² = CF₃; R = Et, R² = C₂F₅], and IV was hydrolyzed to (CF₃)₂CHCONH₂ and CF₃CONEt₂. IR and ¹H and ¹⁹F NMR data were given for all title products.

Zhurnal Obshchei Khimii published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Formula: C6H10F3NO.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kutschy, P. published the artcileReactivity of N’-substituted N-(4-pentynoyl)- and N-[2-(2-propynyl)-4-pentynoyl]thioureas, Category: amides-buliding-blocks, the publication is Chemical Papers (1987), 41(4), 519-26, database is CAplus.

Treatment of HCCCH₂CHRCONHCSNR¹R² (I; R = H, HCCCH₂; R¹, R² = H, Ph; R¹R²N = morpholino) with EtONa and HgCl₂ or Hg(OAc)₂ resp., results in splitting-off the acyl residue and formation of H₂NCSNR¹R². Heating I (R = HCCCH₂, R¹R²N = morpholino) EtOH with a catalytic amount of TiCl₃ gave 58% (HCCCH₂)₂CHCONHCSOEt. Treating I (R = H, HCCCH₂; R¹ = R² = Ph) with Br₂ in CHCl₃ gave 80-87% the benzothiazoline derivatives II (R = H, HCCCH₂).

Chemical Papers published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Fefelova, S. R. published the artcileRegioselective Synthesis of Pyridin-2-One Derivatives Based on Ethyl(1-Phenylethylidene)Cyanoacetate and Cyanoacetamides, HPLC of Formula: 15029-36-4, the publication is Chemistry of Heterocyclic Compounds (New York, NY, United States) (2014), 50(8), 1133-1136, database is CAplus.

Et (1-phenylethylidene)cyanoacetate reacted with cyanoacetamides in an alc. solution of sodium ethoxide, forming various pyridin-2-ones. The cyclization direction of the Michael adducts was affected by the nucleophilicity of the cyanoacetamide used as a CH acid.

Chemistry of Heterocyclic Compounds (New York, NY, United States) published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, HPLC of Formula: 15029-36-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics