Tag: M.W=100-150

Todaro, V. published the artcileDevelopment and characterization of ibuprofen co-crystals granules prepared via fluidized bed granulation in a one-step process – a design of experiment approach, Safety of Isonicotinamide, the publication is Drug Development and Industrial Pharmacy (2021), 47(2), 292-301, database is CAplus and MEDLINE.

The focus of this study was to investigate the possibility of producing ibuprofen-nicotinamide (IBU-NIC) and ibuprofen-isonicotinamide (IBU-INA) cocrystal-containing granules, using a one-step fluidized bed dryer granulation manufacturing process, and evaluate their mech. properties. Pharmaceutical cocrystals represent a suitable strategy to improve properties of active pharmaceutical ingredients (APIs), such as solubility and processability. Ibuprofen (IBU) is a small mol. API which can form cocrystals with different coformers, including NIC and INA. An improvement in mech. properties for IBU-NIC cocrystals relative to IBU was previously reported but, to date, the formulation of IBU cocrystals in a solid dosage form has not been investigated. In situ cocrystn. and granulation were achieved concurrently by processing in a lab-scale fluidized bed granulator following a design of experiment (DoE) approach using a two-level factorial design with both process and formulation variables. Solid-state, micrometric, dissolution, and mech. (tabletability) characteristics of granules were assessed post-processing. Granules containing cocrystals were successfully prepared for 11 of 16 DoE runs. Parameters with a significant effect on granule drug loading, flow function, porosity, and size could be identified from the DoE model. Process yield was increased by using a high inlet temperature at high solution feed rate. To avoid the formation of sticky particles, caking and over-wetting of the powder during the process, the utilization of high inlet temperature, low API + coformer:filler ratio, low API concentration in solution and low solution feed rate were suggested by the model. The multivariable model developed enables accurate optimization of the granulation process for IBU cocrystals.

Drug Development and Industrial Pharmacy published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C5H11BrO, Safety of Isonicotinamide.

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

Keil, D. published the artcileSynthesis and characterization of 1,3-bis-(2-dialkylamino-5-thiazolyl)-substituted squaraines and their 2-(dialkylamino)thiazole precursors, Product Details of C5H10N2OS, the publication is Liebigs Annalen (1995), 979-84, database is CAplus.

By condensing of squaric acid with 2-(dialkylamino)-substituted thiazoles, a novel type of heterocyclic-substituted squaraines was prepared in moderate yield mostly. The squaraines are sparingly soluble in most organic solvents and exhibit narrow absorption bands in the visible range at ∼ 620-700 nm in solution. In dispersed form, the absorption bands of the squaraines are, however, broadened and shifted into the near IR region at ∼ 900 nm. These unique properties of the new squaraines suggest the use of these dyes as spectral sensitizers for laser-driven data recording or data storage media.

Liebigs Annalen 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, Product Details of C5H10N2OS.

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

Czerney, Peter published the artcileHeterocyclic substituted coumarins from β-chloropropeniminium salts, Application of Morpholine-4-carbothioamide, the publication is Journal fuer Praktische Chemie (Leipzig) (1982), 324(2), 255-66, database is CAplus.

The chloropropeniminium salts I (X = N⁺Me₂ ClO₄^–; R = H, 6-Br, 7-OH, 7-OMe, 7-NMe₂, 7-pyrrolidino, 8-OMe, 7-NEt₂, R¹ = H; RR¹ = 5,6-CH:CHCH:CH, 7,8-CH:CHCH:CH) and the aldehydes I (X = O) were prepared by treating 3-acetylcoumarins with DMF-POCl₃ in the presence of HClO₄ or H₂O, resp. I are versatile synthetic intermediates giving I (X = CR²CN, R² = cyano, CO₂Et, 2-benzimidazolyl, 4-O₂NC₆H₄) which were converted to the aminobutadienes. I were also cyclized to pyrylium, thiopyrylium, pyrazolyl, and thiazinyl derivatives

Journal fuer Praktische Chemie (Leipzig) 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, Application of Morpholine-4-carbothioamide.

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

Flaig, Ronald published the artcileSynthesis of N-substituted 2,4-diaminothiazoles and their salts, Product Details of C5H10N2OS, the publication is Heterocycles (1997), 45(5), 875-888, database is CAplus.

A series of N(2),N(4)-substituted 2,4-diaminothiazoles I (R¹R²N = morpholino, pyrrolidino, piperidino, diethylamino, n-butylamino, phenylamino, di-n-propylamino, R³R⁴N = morpholino, pyrrolidino, piperidino, diphenylamino, diethylamino, n-butylamio) and their corresponding mineral acid salts have been prepared by the reaction of POCl₃ with N-substituted S-(dialkylaminocarbonylmethylene)isothiouronium salts R¹R²NC(:NH₂)SCH₂CONR³R⁴ available from corresponding substituted thioureas R¹R²NC(S)NH₂ (II) and N,N-disubstituted chloroacetamides ClCH₂CONR³R⁴ or by the reaction of primary or secondary amines R³R⁴NH in excess with N(2)-unsubstituted or N(2)-disubstituted 2-amino-4-thiazolinimine hydrochlorides III available by the reaction of corresponding N-substituted thioureas II with chloroacetonitrile.

Heterocycles 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, Product Details of C5H10N2OS.

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

Liebscher, Juergen published the artcileReaction of 3-chloroprop-2-eniminium salts with alkali rhodanides, SDS of cas: 14294-10-1, the publication is Zeitschrift fuer Chemie (1978), 18(9), 334-5, database is CAplus.

The pyrimidinethiones I (R = Ph, 4-MeC₆H₄, 4-MeOC₆H₄, 4-ClC₆H₄, 2-naphthyl; R¹ = 4-MeOC₆H₄, 2-MeOC₆H₄, 4-MeC₆H₄, 2-naphthyl, 3-MeOC₆H₄) were obtained by treating RCCl:CHCH:N⁺Me₂ ClO₄^– was alkali metal isothiocyanate and treating SCNCR:CHCH:N⁺Me₂ ClO₄^– (II) with R¹NH₂. Treatment of II with R₂²NH (NR₂² = morpholino, pyrrolidino, NMe₂) gave the thiazinium salts III (R³ = H). Reaction of III (R = 4-MeC₆H₄, NR₂² = NMe₂, R³ = H) with PhNMe₂ gave III (R = 4-MeC₆H₄, NR₂² = NMe₂, R³ = 4-Me₂NC₆H₄).

Zeitschrift fuer Chemie 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, SDS of cas: 14294-10-1.

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

Liebscher, Juergen published the artcileNitrile-formamide adducts. 4. Reaction of nitrile-formamide adducts. Synthesis of N-thioacylamide derivatives and aza analogs of thiopyrylium salts, Safety of Morpholine-4-carbothioamide, the publication is Zeitschrift fuer Chemie (1975), 15(11), 438-40, database is CAplus.

4-RC6H4CSN:CHNR1R2 (R = H, Me, OMe; NR1R2 = pyrrolidino, morpholino, NMe2) were obtained by treating 4-RC6H4CONHCH:N+R1R2 ClO4- with P2S5 or by treating 4-RC6H4CCl:NCH:N+R1R2 ClO4- (I) with Na2S or Na2S2O3. 4-RC6H4CSN:CHNR1R2 were hydrolyzed to 4-RC6H4CSNHCHO or condensed with I (R = H, Cl) to the thiazines II. The thiadiazines III were similarly obtained from I and R4NHCSNR1R2 (R4 = Bz, 4-O2NC6H4CO, 3-O2NC6H4CO, H).

Zeitschrift fuer Chemie 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, Safety of Morpholine-4-carbothioamide.

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

Liebscher, Juergen published the artcileNitrile-formamide chloride adducts; VII. A simple route to 6-N-formamidino-1,3-thiazinium salts, SDS of cas: 14294-10-1, the publication is Zeitschrift fuer Chemie (1976), 16(7), 268-70, database is CAplus.

R3R4N+:CHCR:CClN:CHNR1R2 ClO4-(I; R = Ph, CN, CO2Et, 4-ClC6H4, etc; R1, R2, R3, R4 = Me; R1R2N, R3R4N = morpholino) reacted with R5CSNH2 (R5 = Ph, Me2N, morpholino, PhNH, etc.) to give the thiazinium salts II. I were prepared by the reaction of RCH2CN with dialkylformamide chlorides in the presence of HCl.

Zeitschrift fuer Chemie 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, SDS of cas: 14294-10-1.

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

Mokry, Cornelia published the artcilePreparation and properties of 2-(dialkylamino)-5-(haloacetyl)thiazoles and 4-[2-(dialkylamino)-5-thiazolyl]thiazoles, Application In Synthesis of 14294-10-1, the publication is Journal fuer Praktische Chemie/Chemiker-Zeitung (1998), 340(4), 375-380, database is CAplus.

By the reaction of N-acylthioureas with (ClCH₂)₂CO, 2-(dialkylamino)-5-(chloroacetyl)thiazoles are available. These compounds react with thioureas or arylthioamides under heterocyclization to give bis[2-(dialkylamino)-5-thiazolyl]methanones, 2-aryl-4-[2-(dialkylamino)-5-thiazolyl]thiazoles, or 2-(dialkylamino)-4-[2-(dialkylamino)-5-thiazolyl]thiazoles, resp., from which the latter exhibit a high reactivity towards several electrophilic reagents. Thus, deeply colored cyanovinyl-, arylazo-, and arylmethine-substituted bisthiazole dyes formed.

Journal fuer Praktische Chemie/Chemiker-Zeitung 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, Application In Synthesis of 14294-10-1.

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

Mohammady, Mohsen published the artcileDesign of ultra-fine carvedilol nanococrystals: Development of a safe and stable injectable formulation, Synthetic Route of 1453-82-3, the publication is European Journal of Pharmaceutics and Biopharmaceutics (2021), 139-151, database is CAplus and MEDLINE.

Carvedilol (CAR) is a strategic beta-blocker agent which its application has been limited by its very low water solubility The present study describes a soluble form of drug based on nano-cocrystal (NCC) anti-solvent precipitation technique. The COSMOquick software was employed to select the optimum coformer (tartaric acid, TA) and organic solvent (acetone) relying on the enthalpy changes of cocrystn. and solubilization. Central Composite Design (CCD) considering the impact of CAR, TA, poloxamer 188 (stabilizer) concentrations, and anti-solvent/solvent ratio on CAR NCCs particle size (PS) could produce ultra-fine NCCs (about 1 nm). The lyophilization of NCCs investigating slow/fast freezing rates, various types and concentrations of cryprotectants and lyoprotectants indicated that PEG and trehalose (5% w/v concentration) under slow freezing rate could re-produce the initial PSs successfully. CAR NCCs indicated about 2000 fold increase in solubility compared with pure CAR. DSC and PXRD experiments proved that the formulations containing trehalose led to more crystalline and the ones comprising PEG led to more amorphous structures. Interestingly, the slow freezed PEG protected NCCs were phys. stable for at least 18 mo. In conclusion, the NCC technol. could produce the first safe soluble form of CAR for treating hypertension urgencies easy for industrial scale-up.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Synthetic Route of 1453-82-3.

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

Certal, Victor published the artcilePreparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors, Related Products of amides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(6), 1506-1510, database is CAplus and MEDLINE.

In the authors’ continuous efforts to identify and develop novel targeted cancer treatments, a new morpholino-thiazole scaffold active against PI3Kβ was identified. This Letter reports the optimization of this compound class to develop PI3Kβ isoform-selective inhibitors with suitable pharmacol. properties.

Bioorganic & Medicinal Chemistry Letters 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, Related Products of amides-buliding-blocks.

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