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JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 04/2019, Volume 62, Issue 7, pp. 3228 - 3250
Bruton's tyrosine kinase (BTK), a non-receptor tyrosine kinase, is a member of the Tec family of kinases and is essential for B cell receptor (BCR) mediated... 
RESPONSES | ACTIVATION | DESIGN | CHEMISTRY, MEDICINAL | B-CELL | IBRUTINIB | MICE | ARTHRITIS | ACALABRUTINIB
Journal Article
Organic Process Research & Development, ISSN 1083-6160, 09/2018, Volume 22, Issue 9, pp. 1276 - 1281
An optimized large-scale synthesis of (2S,3aR,7aS)-tert-butyl hexahydro-2,5-methanopyrrolo­[3,2-c]­pyridine-1­(4H)-carboxylate (1A), an important intermediate... 
Sonogashira coupling | iodination | hydrogenation | debenzylation | CHEMISTRY, ORGANIC | CHEMISTRY, APPLIED
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 11/2018, Volume 59, Issue 48, pp. 4267 - 4271
A number of cyanomethyl esters of natural/unnatural aminoacids with un-protected amino functionality were synthesized because of their synthetic and medicinal... 
Cyanomethyl | Aminoacids | Aminoacylation | tRNA analogs | N-Boc | Deprotection | ENZYMES | PDCPA | CHEMISTRY, ORGANIC | AGENTS | UBER AKTIVIERTE ESTER | Amino acids | Dioxane | Amines | Transfer RNA | Organic compounds
Journal Article
Synthesis, ISSN 0039-7881, 02/2020, Volume 52, Issue 3, pp. 441 - 449
Abstract An efficient and practical synthetic protocol for the synthesis of 1,4-disubstituted pyrrolo[1,2- a ]pyrazine derivatives is described that originates... 
paper
Journal Article
Synthesis, ISSN 0039-7881, 11/2017, Volume 49, Issue 22, pp. 5039 - 5044
Abstract A short and scalable process for the preparation of multi-gram quantities of orthogonally protected bis(aminomethyl)malonic acid in good yield from... 
paper | improved process | macrocyclic peptides | benzyl ethyl malonate | BUILDING-BLOCKS | gram scale synthesis | CHEMISTRY, ORGANIC | SOLID SUPPORT | CYCLIC-PEPTIDES | OLIGONUCLEOTIDES | PEPTIDOMIMETICS | AMINO-ACIDS | CONSTRUCTION | CHEMISTRY | SCAFFOLDS | orthogonally protected amino acid | N-2-ALKYL-1,2,3,4-TETRAHYDROISOQUINOLINES
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2016, Volume 59, Issue 19, pp. 9173 - 9200
Journal Article
Organic Process Research & Development, ISSN 1083-6160, 10/2016, Volume 20, Issue 10, pp. 1717 - 1720
An enantioselective synthesis of (S)-7-amino-5H,7H-dibenzo­[b,d]­azepin-6-one (S-1) is described. The key step in the sequence involved crystallization-induced... 
3 5-dichlorosalicylaldehyde | Notch inhibitors | DKR | CIDR | Alzheimers disease | Boc-D-phenylalanine | dibenzoazepenone | LY411575 | 3,5-dichlorosalicylaldehyde | ALZHEIMERS-DISEASE | CHEMISTRY, ORGANIC | KINETIC RESOLUTION | INDUCED ASYMMETRIC TRANSFORMATION | LACTAMS | CHEMISTRY, APPLIED | Alzheimer's disease
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2015, Volume 58, Issue 22, pp. 9010 - 9026
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2020, Volume 30, Issue 1, p. 126782
Uncialamycin is one of the structurally simpler and newer members of enediyne family of natural products. It exhibits highly potent activity against several... 
Antibody-drug conjugate (ADC) | Linker | Enediyne | Uncialamycin | Cancer | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2016, Volume 59, Issue 17, pp. 8042 - 8060
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 05/2015, Volume 25, Issue 9, pp. 1905 - 1909
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 05/2017, Volume 60, Issue 9, pp. 3795 - 3803
Journal Article
ORGANIC PROCESS RESEARCH & DEVELOPMENT, ISSN 1083-6160, 05/2019, Volume 23, Issue 5, pp. 912 - 918
A scalable route to 1-(5-(4-(3-hydroxy-3-methylbutyl)-1H-1,2,3-triazol-1-yl)-4-(isopropylamino)pyridin-2-yl)-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (1,... 
kinase inhibitor | 1H-pyrazolor[3,4-b]pyridine derivative | HYDRAZINE | REDUCTION | 1,2,3-TRIAZOLES | DSC studies | CHEMISTRY, ORGANIC | scalable synthesis | CHEMISTRY, APPLIED | azide | triazole | RATIONAL DESIGN
Journal Article
Organic Process Research & Development, ISSN 1083-6160, 07/2018, Volume 22, Issue 7, pp. 846 - 855
This paper describes the efficient scale-up synthesis of the potent negative allosteric glutamate N2B (GluN2B) inhibitor 1 (BMS-986169), which relies upon a... 
PNA | ANALOGS | STABILITY | TRIFLUORIDE | CHEMISTRY, ORGANIC | NEGATIVE ALLOSTERIC MODULATOR | DEPRESSIVE-DISORDERS | CHEMISTRY, APPLIED
Journal Article
Journal of medicinal chemistry, ISSN 0022-2623, 01/2020
Factor XIa (FXIa) inhibitors are promising novel anticoagulants, which show excellent efficacy in preclinical thrombosis models with minimal effects on... 
Journal Article
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