- Well-Defined Poly(Ester Amide)-Based Homo- and Block Copolymers by One-Pot Organocatalytic Anionic Ring-Opening Copolymerization of N-Sulfonyl Aziridines and Cyclic Anhydrides
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We report a new synthetic methodology for poly(ester amide)s by anionic ring-opening copolymerization of N-sulfonyl aziridines and cyclic anhydrides. Phosphazenes organocatalysts have been found to promote a highly-active, controlled, and selective altern
- Xu, Jiaxi,Hadjichristidis, Nikos
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p. 6949 - 6954
(2021/03/01)
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- Modular One-Step Three-Component Synthesis of Tetrahydroisoquinolines Using a Catellani Strategy
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Reported is a modular one-step three-component synthesis of tetrahydroisoquinolines using a Catellani strategy. This process exploits aziridines as the alkylating reagents, through palladium/norbornene cooperative catalysis, to enable a Catellani/Heck/aza-Michael addition cascade. This mild, chemoselective, and scalable protocol has broad substrate scope (43 examples, up to 90 % yield). The most striking feature of this protocol is the excellent regioselectivity and diastereoselectivity observed for 2-alkyl- and 2-aryl-substituted aziridines to access 1,3-cis-substituted and 1,4-cis-substituted tetrahydroisoquinolines, respectively. Moreover, this is a versatile process with high step and atom economy.
- Qian, Guangyin,Bai, Miao,Gao, Shijun,Chen, Han,Zhou, Siwei,Cheng, Hong-Gang,Yan, Wei,Zhou, Qianghui
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p. 10980 - 10984
(2018/07/30)
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- Synthesis of indolines: Via a palladium/norbornene-catalyzed reaction of aziridines with aryl iodides
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A Pd- and norbornene-catalyzed domino procedure has been developed to synthesize indoline compounds. This reaction provides efficient access to indolines by employing aryl iodides with aziridines as new electrophiles. The transformation is scalable and tolerates a range of functional groups.
- Liu, Ce,Liang, Yujie,Zheng, Nian,Zhang, Bo-Sheng,Feng, Yuan,Bi, Siwei,Liang, Yong-Min
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supporting information
p. 3407 - 3410
(2018/04/05)
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- NOVEL OXAZOLE DERIVATIVES THAT INHIBIT SYK
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The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases s
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- DIAZASPIROALKANEONE-SUBSTITUTED OXAZOLE DERIVATIVES AS SPLEEN TYROSINE KINASE INHIBITORS
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The present invention is concerned with diazaspiroalkanone- substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human a
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- Mimics of small ribozymes utilizing a supramolecular scaffold
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For elucidating the mechanism of the general acid/base catalysis of the hydrolysis of RNA phosphodiester bonds, a number of cleaving agents having two cyclen moieties tethered to a 1,3,5-triazine core have been prepared and their ability to bind and cleave uridylyl-3′,5′-uridine (UpU) studied over a wide pH range. Around neutral pH, the cleaving agents form a highly stable ternary complex with UpU and Znii through coordination of the uracil N3 and the cyclen nitrogen atoms to the Znii ions. Under conditions where the triazine core exists in the deprotonated neutral form, hydrolysis of UpU, but not of adenylyl-3′,5′-adenosine (ApA), is accelerated by approximately two orders of magnitude in the presence of the cleaving agents, suggesting general base rather than metal ion catalysis. The probable mechanism of the observed catalysis and implications to understanding the general acid/base-catalyzed phosphodiester hydrolysis by ribozymes are discussed. The Royal Society of Chemistry 2012.
- Loennberg, Tuomas A.,Helkearo, Mia,Jancso, Attila,Gajda, Tamas
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p. 3328 - 3338
(2012/04/10)
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- Development of hypoxia-sensitive Gd3+-based MRI contrast agents
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Hypoxia occurs in various diseases, including cancer, ischemia, and acute and chronic vascular diseases. Here we describe the design and synthesis of the first hypoxia-sensitive MRI contrast agents, SAGds. SAGds showed a pH-dependent r1 relaxivity change associated with intramolecular chelation of the nitrogen atom of the sulfonamide moiety to the Gd3+ center. There was a correlation between the pKa of the r1 relaxivity change and the sum of the Hammett σ constants of substituents on the aromatic ring. Among the synthesized compounds, 4NO22MeOSAGd was selectively reduced to the amine by rat liver microsomes under hypoxic conditions, resulting in a 1.8-fold increment of the r1 relaxivity owing to the change in pKa of the arylsulfonamide moiety. This enhancement of the r 1 relaxivity could be clearly detected in T1-weighted MR images. Thus, 4NO22MeOSAGd is a 'smart' MRI contrast agent for the detection of hypoxia under physiological conditions.
- Iwaki, Shimpei,Hanaoka, Kenjiro,Piao, Wen,Komatsu, Toru,Ueno, Tasuku,Terai, Takuya,Nagano, Tetsuo
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p. 2798 - 2802
(2012/06/01)
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- The Zn2+ complex of 1,4,7,10-tetraazacyclododecane as an artificial nucleobase
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{2-Deoxy-3-O-[2-cyanoethoxy(diisopropylamino)phosphino]-5-O-(4, 4'-dimethoxytrityl)-D-erythro-pentofuranosyl}-N-{2-[4,7,10-tris(2,2, 2-trifluoroacetyl)-1,4,7,10-tetraazacyclododecan-1-yl]ethyl}acetamide (1) was prepared and incorporated into a 2'-O-methyl oligoribonucleotide. The hybridization of this oligonucleotide with complementary 2'-O-methyl oligoribonucleotides incorporating one to five uracil bases opposite to the azacrown structure was studied in the absence and presence of Zn2+. Introduction of Zn2+ moderately stabilized the duplex with U-bulged targets. Copyright Taylor and Francis Group, LLC.
- Laine, Maarit,Aromaa, Maria,Virta, Pasi,Lonnberg, Tuomas,Poijaervi-Virta, Paeivi,Loennberg, Harri
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experimental part
p. 609 - 618
(2011/12/15)
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- HETEROCYCLIC MODULATORS OF PKB
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The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
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Page/Page column 131-132
(2009/03/07)
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