1 As of December 2018, acalabrutinib has been administered to over 3,500 participants in clinical studies, including subjects with hematologic malignancies and solid tumors. In the human CLL NSG xenograft model, Acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferationAcalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activityRoom temperature in continental US; may vary elsewhere.Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)Please fill out this form to request the QC report. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. 589, North Yulong Road, Chunjiang Town, Xinbei District, Changzhou, 213127 Jiangsu, ChinaPharmaceutical Technology and Development, AstraZeneca, Silk Road Business Park, Macclesfield SK10 2NA, United KingdomChangzhou SynTheAll Pharmaceutical Co., Ltd., No. Synthesis of acalabrutinib, using 3-chloropyrazine-2-carbonitrile as the starting material, is described. 9g, 8.9mmol), methyl tert-butyl ether (IOOmL) and water (40 mL) was added a reaction flask, the reaction mixture was heated to 100 ° C the reaction was stirred for 12h, the reaction was cooled to room temperature, and concentrated by rotary evaporation to dryness, was added acetic acid extracted with ethyl, brine, dried over magnesium sulfate, and concentrated by rotary evaporation to dryness, a mixed solvent of ethyl acetate and n-hexane and recrystallized to give ⑸-2- {8- tert-butoxycarbonyl-amino-1- [4- (2 – pyridin-ylcarbamoyl) phenyl] imidazo [I, 5-a] pyrazin-3-yl} -1-pyrrolidine-carboxylate, an off-white solid (3.9 g of), in 79% yield, this step the reaction scheme in Example 1. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Synthesis of acalabrutinib, using 3-chloropyrazine-2-carbonitrile as the starting material, is described. As the situation with COVID-19 continues to unfold in every communities, MedChemExpress is responding to the uncertainty caused by this outbreak thoughtfully and cautiously. Optimization and application of the reported synthesis of (3-chloropyrazin-2-yl)methanamine 3 have provided a high yielding, fully telescoped procedure to key intermediate 5 in the synthesis of acalabrutinib. 4g, IOmmol), bis (triphenylphosphine) dichloride Leba (0.41g, 0.58mmol), potassium phosphate (I. As of 2019, it was unclear whether it improved outcomes. Acalabrutinib has not been associated with serum enzyme elevations during therapy or with cases of idiosyncratic acute liver injury, but has been linked to cases of reactivation of hepatitis B. Your need for high quality reagent doesn't stop during difficult times, and neither do we.
[0077] (6) Preparation of (S) -2- {8- tert-butoxycarbonyl-amino-1- [4- (2-carbamoyl-pyridyl) phenyl] imidazo [1, 5-a] pyrazine 3-yl} -1- (2-butynoyl) pyrrolidine:[0078] (S) -2- {8- tert-butoxycarbonyl-amino-1- [4- (2-carbamoyl-pyridyl) phenyl] imidazo [I, 5-a] pyrazin-3-yl } ratio slightly burning Jie (2.5g, 5mmol) was dissolved in toluene (50 mL), with stirring, was added 2-butyne chloride (0.62g, 6mmol), was added dropwise N, N- dimethylaniline (Ig, 8.5mmo 1), The reaction mixture was 40 ° C the reaction was stirred for 12h, the reaction solution was concentrated by rotary evaporation to dryness, dilute hydrochloric acid was added was adjusted to neutral, extracted with ethyl acetate was added, dried over magnesium sulfate, and concentrated by rotary evaporation to dryness, and recrystallized from methanol to give ⑸-2- {8-tert-butoxycarbonyl-amino-1- [4- (2-carbamoyl-pyridyl) phenyl] imidazo [I, 5-a] pyrazin-3-yl} -1- (2-butyn acyl) pyrrolidine-white solid (2.5g), 88% yield, this step is the same reaction scheme as in Example 1.
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation Article Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. We do not sell to patients. Acalabrutinib (ACP-196) is a more selec - tive, irreversible BTK inhibitor that is specifically designed to improve on the safety and efficacy of first-generation BTK inhibitors. Acalabrutinib, also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. We're doing our best to keep everyone healthy and safe in the workplace while also avoiding the interruptions to our day-to-day operations. [0075] (5) Preparation of (S) -2- {8- tert-butoxycarbonyl-amino-1- [4- (2-carbamoyl-pyridyl) phenyl] imidazo [1, 5_a] pyrazin-3 -} pyrrolidine:[0076] (S) -2- {8- tert-butoxycarbonyl group -I- [4- (2- carbamoyl-pyridyl) phenyl] imidazo [I, 5-a] pyrazin-3-yl } -1 Jie section than slightly burning acid ester (3.5g, 5.5mmol) was dissolved in ethanol (50mL), was added cesium charcoal (0.2g), under a hydrogen pressure into 45 ° C the reaction 6h.Concentrated suction through Celite to remove the catalyst and the filtrate was rotary evaporated to dryness to afford ⑸-2- {8- tert-butoxycarbonyl-amino-1- [4- (2-carbamoyl-pyridyl) phenyl] imidazo [ I, 5-a] pyrazin-3-yl} pyrrolidine as a white solid powder (2.6 g of), in 95% yield, this step is the same reaction scheme as in Example 1. Acalabrutinib (trade name Calquence) is a medication used to treat a type of non-Hodgkin lymphoma known as mantle cell lymphoma. You have to login with your ACS ID befor you can login with your Mendeley account.Changzhou SynTheAll Pharmaceutical Co., Ltd., No. Acalabrutinib blocks the action of certain enzymes in the body, which can interfere with the growth and spread of cancer cells.
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