70930-18-6Relevant articles and documents
Asymmetric Synthesis of N-Boc-(R)-Silaproline via Rh-Catalyzed Intramolecular Hydrosilylation of Dehydroalanine and Continuous Flow N-Alkylation
Chung, John Y. L.,Shevlin, Michael,Klapars, Artis,Journet, Michel
, p. 1812 - 1815 (2016)
An asymmetric synthesis of a silicon-containing proline surrogate, N-Boc-(R)-silaproline (1), is described. Starting from N-Boc-dehydroalanine ester, deprotonation, followed by N-alkylation with chloromethyldimethylsilane under flow conditions, afforded the N-alkylated product 8 in 91% yield. An unprecedented enantioselective (NBD)2RhBF4/Josiphos 404-1 catalyzed 5-endo-trig hydrosilylation afforded the silaproline ester in 85-90% yield and >95% ee. Subsequent saponification and salt formation upgraded 1 to >99% ee.
ALGINIC ACID DERIVATIVE BONDED TO NONSTEROIDAL ANTI-INFLAMMATORY COMPOUND
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Paragraph 0158; 0343-0344, (2021/01/26)
Provided is water-soluble compound that can be used in a sustained-release preparation and is capable of stably releasing a fixed amount of an active ingredient in vivo by using the novel potential base material option of alginic acid as the base material
Synthesis and Diversification of Macrocyclic Alkynediyl Sulfide Peptides
Godin, éric,Nguyen Thanh, Sacha,Guerrero-Morales, Javier,Santandrea, Jeffrey,Caron, Antoine,Minozzi, Clémentine,Beaucage, Noémie,Rey, Bastien,Morency, Mathieu,Abel-Snape, Xavier,Collins, Shawn K.
supporting information, p. 14575 - 14579 (2020/10/12)
The synthesis of rare macrocyclic alkynediyl sulfides by a Cu-catalyzed Csp?S cross-coupling is presented. The catalytic protocol (Cu(MeCN)4PF6/dtbbpy) promotes macrocyclization of peptides, dipeptides and tripeptides at ambient temperature (14 examples, 23→73 % yields) via thiols and bromoalkynes, and is chemoselective with regards to terminal alkynes. Importantly, the underexplored alkynediyl sulfide functionality incorporates a rigidifying structural element and opens new opportunities for diversification of macrocyclic frameworks through S oxidation, halide addition and azide–alkyne cycloaddition chemistries to integrate sulfones, halides or valuable fluorophores (7 examples, 37→92 % yields).
TRICYCLIC COMPOUNDS AND THEIR USE
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Page/Page column 86, (2020/12/29)
Tricyclic compounds and their use are provided. More specifically, tricyclic compounds, pharmaceutical compositions containing them, methods for preparing them, and their use in therapy are also provided.
Cycloaddition Strategies for the Synthesis of Diverse Heterocyclic Spirocycles for Fragment-Based Drug Discovery
King, Thomas A.,Stewart, Hannah L.,Mortensen, Kim T.,North, Andrew J. P.,Sore, Hannah F.,Spring, David R.
, p. 5219 - 5229 (2019/08/12)
In recent years the pharmaceutical industry has benefited from the advances made in fragment-based drug discovery (FBDD) with more than 30 fragment-derived drugs currently marketed or progressing through clinical trials. The success of fragment-based drug
GLYCOSAMINOGLYCAN DERIVATIVE AND METHOD FOR PRODUCING SAME
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Paragraph 0449-0452, (2016/06/28)
The present invention provides a glycosaminoglycan derivative in which a group derived from glycosaminoglycan and a group derived from a physiologically active substance having at least one of a carboxy group and a hydroxy group are coupled by covalent bond with a spacer therebetween, in which the spacer is selected in accordance with the decomposition rate of the covalent bond to the group derived from the physiologically active substance.
NOVEL PSYCHOTROPIC AGENTS HAVING GLUTAMATE NMDA ACTIVITY
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Page/Page column 36; 37, (2008/12/05)
The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.
Peptide-bond modified glutathione conjugate analogs modulate GSTπ function in GSH-conjugation, drug sensitivity and JNK signaling
Burg, Danny,Riepsaame, Joey,Pont, Chantal,Mulder, Gerard,Van De Water, Bob
, p. 268 - 277 (2007/10/03)
Glutathione S-transferase π (GST, E.C.2.5.1.18) overexpression contributes to resistance of cancer cells towards cytostatic drugs. Furthermore, GSTπ is involved in the cellular stress response through inhibition of Jun N-terminal-kinase (JNK), a process t
The Baylis-Hillman reaction with chiral α-amino aldehydes under racemization-free conditions
Coelho, Fernando,Diaz, Gaspar,Abella, Carlos A. M.,Almeida, Wanda P.
, p. 435 - 439 (2007/10/03)
The Baylis-Hillman reaction with chiral α-amino aldehydes has been revisited. The reaction carried out under the influence of ultrasound avoids the aldehyde racemization almost completely, providing useful chiral substrates which can be used as starting materials for the synthesis of natural products. To demonstrate the synthetic applicability of these adducts, the easy preparation of a bicyclic lactam with an indolizidinic skeleton was accomplished. Georg Thieme Verlag Stuttgart.
A mild and effective method for the transesterification of carboxylic acid esters
Baumhof, Patrick,Mazitschek, Ralph,Giannis, Athanassios
, p. 3672 - 3674 (2007/10/03)
An extraordinarily versatile transesterification of simple or highly functionalized esters of aliphatic and aromatic carboxylic acids in high yields is catalyzed by dibutyltin oxide [Eq. (1)]. The reaction is compatible with several functional groups, for example, acetals, ketals, aliphatic bromides, enol ethers, urethanes, as well as free hydroxy, phenolic, and amino groups, and even with water.
