141973-57-1Relevant articles and documents
A DNA-Encoded Chemical Library Incorporating Elements of Natural Macrocycles
Stress, Cedric J.,Sauter, Basilius,Schneider, Lukas A.,Sharpe, Timothy,Gillingham, Dennis
supporting information, p. 9570 - 9574 (2019/06/24)
Here we show a seven-step chemical synthesis of a DNA-encoded macrocycle library (DEML) on DNA. Inspired by polyketide and mixed peptide-polyketide natural products, the library was designed to incorporate rich backbone diversity. Achieving this diversity, however, comes at the cost of the custom synthesis of bifunctional building block libraries. This study outlines the importance of careful retrosynthetic design in DNA-encoded libraries, while revealing areas where new DNA synthetic methods are needed.
INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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Paragraph 398, (2015/05/05)
The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g.,leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. (I)
A novel synthesis of 1,3-benzodiazepin-2-ones using intramolecular heck reaction
Hayashi, Masahito,Sai, Hiroshi,Horikawa, Hiroshi
, p. 1331 - 1335 (2007/10/03)
The formation of the skeleton of 1,3-benzodiazepin-2-one could be efficiently achieved by intramolecular Heck reaction. This methodology was well applicable to the preparation of optically pure 4-substituted 1,3-benzodiazepin-2-ones starting from easily available α-amino acids.
Reaction of azides with trimethyl phosphite in the presence of water: a chemoselective synthesis of functionalized phosphoramidates
Zidani, A.,Carrie, R.,Vaultier, M.
, p. 71 - 75 (2007/10/02)
The reductive phosphorylation of azides with trimethyl phosphite and water in THF leads to the corresponding phosphoramidates which are protected primary amines in excellent yields.The P-N bond in these derivatives may be easily cleft in acidic medium to give the primary amine salts.Some examples are reported.The bis-anion 4 obtained by metallation of 3b is C-alkylated at low temperature leading to new phosphoramidates. 3i and 3j derived from α-azidoketones could not be transformed into the corresponding α-aminoketone salts.The use of methyl diphenylphosphinite in place of trimethyl phosphite leads to the diphenylphosphinamide 7 which, when treated with para-toluenesulfonic acid monohydrate in ether, gives the corresponding α-aminoacetone salt 8 in good yield.Keywords: azides / reductive phosphorylation / phosphoramidates / chemoselective reduction / functionalized primary amines