- A facile synthesis of bicyclo[4.2.0]octa-1,3,5-trien-3-ol
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Bicyclo[4.2.0]octa-1,3,5-trien-3-ol (2) has been synthesized in good yield via a Baeyer-Villiger reaction of the corresponding aldehyde 5 with permonophosphoric acid.
- Thomas,Pews
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- A facile approach to architecturally defined nanoparticles via intramolecular chain collapse
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A novel approach is presented for the controlled intramolecular collapse of linear polymer chains to give well-defined single-molecule nanoparticles whose structure is directly related to the original linear polymer. By employing a combination of living free radical polymerization and benzocyclobutene (BCB) chemistry, nanoparticles can be routinely prepared in multigram quantities with the size being accurately controlled by either the initial degree of polymerization of the linear chain or the level of incorporation of the BCB coupling groups. The latter also allows the cross-link density of the final nanoparticles to be manipulated. In analogy with dendritic macromolecules, a significant reduction of up to 75% in the hydrodynamic volume is observed on going from the starting random coil linear chains to the corresponding nanoparticles. The facile nature of the living free radical process also permits wide variation in monomer selection and functional group incorporation and allows novel macromolecular architectures to be prepared. Furthermore, the use of block copolymers functionalized with benzocyclobutene groups in only one of the blocks gives, after intramolecular collapse, a hybrid architecture in which a single linear polymer chain is attached to the globular nanoparticle.
- Harth, Eva,Van Horn, Brooke,Lee, Victor Y.,Germack, David S.,Gonzales, Chad P.,Miller, Robert D.,Hawker, Craig J.
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- First synthesis of optically active benzocyclobutene and biphenylene-based unusual α-amino acid derivatives
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Various optically pure benzocyclobutene and biphenylene-based α-amino acid derivatives are prepared in a very high diastereoselective manner via a six step sequence using Schollkopf chiral auxiliary.
- Kotha, Sambasivarao,Sreenivasachary, Nampally,Halder, Somnath
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- SULFONIMIDAMIDE COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: (Formula AA) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
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Page/Page column 474-475
(2020/08/13)
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- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
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Page/Page column 286-287
(2020/06/05)
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- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured.The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.
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Page/Page column 512; 513
(2019/02/13)
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- FULLERENE DERIVATIVES
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A fullerene derivative having a partial structure represented by formula (1): wherein R represents a monovalent group, and r represents an integer of 0 to 4, in particular, a fullerene derivative, which has one to four structures represented by formula (1), can be applied to an organic photoelectric conversion element having a high open-circuit voltage and is therefore suitable for an organic thin-film solar cell or an organic photosensor, and thus it is extremely useful.
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Page/Page column 11
(2012/06/18)
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- DENDRITIC MOLECULAR INTRACELLULAR TRANSPORTERS AND METHODS OF MAKING AND USING SAME
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In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to compounds comprising the structure: and at least one guanidinium residue, wherein m is zero or a positive integer. Also disclosed are methods of preparing the disclosed compounds. Also disclosed are methods of intracellular delivery comprising administering the disclosed compounds and compositions to a subject. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of one or more compounds or compositions of the invention and a pharmaceutically acceptable carrier. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Page/Page column 94-95
(2010/11/30)
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- Synthesis of optically active benzocyclobutene and biphenylene based unusual α-amino acid derivatives
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Optically active benzocyclobutene and biphenylene based unusual α-amino acid derivatives have been prepared via a six step sequence using Schoellkopf chiral auxiliary in a very high diastereoselective manner.
- Kotha, Sambasivarao,Halder, Somnath
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p. 863 - 872
(2007/10/03)
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- Process for preparing hydroxyalkylbenzocyclobutenes
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A process for preparing a substituted or unsubstituted 3- or 4-hydroxyalkylbenzocyclobutene compound comprises reducing a corresponding 3- or 4-formyl or ketobenzocyclobutene compound with a hydride at a temperature below that at which dimerization or oligomerization of the formyl- or ketobenzocycloutene compound or the thus-produced hydroxyalkylbenzocyclobutene compound is a significant side reaction, for a time sufficient to convert the formyl- or ketobenzocyclobutene compound to the hydroxyalkylbenzocyclobutene compound. In a two-step process, formylbenzocyclobutenes are prepared from bromobenzocyclobutenes in 90% yield or from benzocyclobutenes in a 70% yield, and then converted to hydroxymethylbenzocyclobutenes for an overall yield of about 85% from a bromobenzocyclobutene or of about 65% from a benzocyclobutene. In a two-step process, ketobenzocyclobutenes from bromobenzocyclobutene Grignard reagents and an N-alkanoyl- or N-aroyl-2-methylaziridine are converted to hydroxyalkylbenzocyclobutenes in high yields.
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