65595-02-0Relevant academic research and scientific papers
COMPOUNDS, COMPOSITIONS AND METHODS FOR SYNTHESIS
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, (2019/01/10)
The present disclosure, among other things, provides technologies for synthesis, including reagents and methods for stereoselective synthesis. In some embodiments, the present disclosure provides compounds useful as chiral auxiliaries. In some embodiments, the present disclosure provides reagents and methods for oligonucleotide synthesis. In some embodiments, the present disclosure provides reagents and methods for chirally controlled preparation of oligonucleotides. In some embodiments, technologies of the present disclosure are particularly useful for constructing challenging internucleotidic linkages, providing high yields and stereoselectivity.
One-pot conversion of alkyl aldehydes into substituted propanoic acids via Knoevenagel condensation with Meldrum's acid
Mudhar, Harminder,Witty, Andrew
experimental part, p. 4972 - 4974 (2011/01/12)
Reaction of a range of alkyl aldehydes and Meldrum's acid in triethylammonium formate (TEAF) at 100 °C generates substituted propanoic acids in a single step.
Inter- and intramolecular addition reactions of electron-deficient alkenes with alkyl radicals, generated by SET-photochemical decarboxylation of carboxylic acids, serve as a mild and efficient method for the preparation of γ-amino acids and macrocyclic l
Yoshimi, Yasuharu,Masuda, Miho,Mizunashi, Tomoyuki,Nishikawa, Keisuke,Maeda, Kousuke,Koshida, Nobumasa,Itou, Tatsuya,Morita, Toshio,Hatanaka, Minoru
supporting information; experimental part, p. 4652 - 4655 (2009/12/24)
Inter- and Intramolecular additions of alkyl radicals, generated by SET photochemical decarboxylation reactions of free carboxylic acids, to electron-deficient alkenes take place under mild conditions as part of efficient routes for the formation of NBoc
TRICYCLIC COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE
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Page/Page column 41-42, (2010/02/14)
A compound of the formula: wherein R1 is a 5- or 6-membered ring; ???Z1 is a 5- or 6-membered aromatic ring; ???Z2 is a group of -Z2a-W2-Z2b-, wherein Z2a and Z2b are each O, S(O)q (wherein q is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain; ???W is a group represented by wherein R3 and R3' are each a hydrogen atom, a lower alkyl group, or a lower alkoxy group; X is CH or N; n and n' are each an integer of 0 or 1 to 4; m and m' are each 1 or 2; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a lower alkyl group, or a lower acyl group); and ???R2 is (1) an amino group, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atommay be converted to a quaternary ammonium or an oxide; or a salt thereof. The compound exhibits excellent CCR antagonist activity against CCR5, and is useful as a prophylactic and/or therapeutic agent for HIV infection in human peripheral blood mononuclear cells, especially for AIDS.
A synthesis of the tetracyclic carboskeleton of isaindigotidione
Poon, Ch. Yan,Chiu, Pauline
, p. 2985 - 2988 (2007/10/03)
An efficient synthesis of the unique indolizino[7,6-c]quinoline carboskeleton of isaindigotidione has been achieved. This strategy employed L-proline and isatin as the main building blocks in the construction of the framework. Four transformations occurred in a one-pot operation to furnish the tetracyclic nucleus.
Trifluoroacetic acid-mediated intramolecular formal N-H insertion reactions with amino-α-diazoketones: A facile and efficient synthesis of optically pure pyrrolidinones and piperidinones
Yang, Hua,Jurkauskas, Valdas,Mackintosh, Nicole,Mogren, Tobias,Stephenson, Corey R. J.,Foster, Katherine,Brown, William,Roberts, Edward
, p. 800 - 808 (2007/10/03)
Trifluoroacetic acid (TFA) was found to promote intramolecular formal N-H insertion reactions. Upon treatment with TFA, optically pure N-Boc-β′-amino-α-diazoketones (5a-c) and N-Boc-γ′-amino-α-diazoketones (10a-d) can be converted, with retention of chira
Synthesis and antitumor activity of novel dolastatin 10 analogs
Miyazaki,Kobayashi,Natsume,Gondo,Mikami,Sakakibara,Tsukagoshi
, p. 1706 - 1718 (2007/10/03)
Dolastatin 10 (1) is a potent antineoplastic pentapeptide. Novel dolastatin 10 analogs each modified at one of the constituent amino acid derivatives, were synthesized and their antitumor activity was evaluated against P388 leukemia in mice. The structural requirements for antitumor activity are discussed. Some of the analogs, 31c, 35c, 38b, and 50c showed excellent activity in vivo. Highly active 50c, which lacks the thiazole group of 1, was selected for further development as an antitumor agent.
