- An improved synthesis of 3-aminoestrone
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An efficient Pd(0)-catalyzed protocol for the rapid and efficient preparation of 3-aminoestrone via 3-benzylaminoestrone from estrone-triflate is described. The three step synthesis proceeds with an overall yield of about 55% using X-Phos as optimal ligan
- Sch?n, Uwe,Messinger, Josef,Buchholz, Monika,Reinecker, Uwe,Thole, Hubert,Prabhu, Manoj K. S.,Konda, Ashok
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- Light- and Manganese-Initiated Borylation of Aryl Diazonium Salts: Mechanistic Insight on the Ultrafast Time-Scale Revealed by Time-Resolved Spectroscopic Analysis
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Manganese-mediated borylation of aryl/heteroaryl diazonium salts emerges as a general and versatile synthetic methodology for the synthesis of the corresponding boronate esters. The reaction proved an ideal testing ground for delineating the Mn species responsible for the photochemical reaction processes, that is, involving either Mn radical or Mn cationic species, which is dependent on the presence of a suitably strong oxidant. Our findings are important for a plethora of processes employing Mn-containing carbonyl species as initiators and/or catalysts, which have considerable potential in synthetic applications.
- Firth, James D.,Hammarback, L. Anders,Burden, Thomas J.,Eastwood, Jonathan B.,Donald, James R.,Horbaczewskyj, Chris S.,McRobie, Matthew T.,Tramaseur, Adam,Clark, Ian P.,Towrie, Michael,Robinson, Alan,Krieger, Jean-Philippe,Lynam, Jason M.,Fairlamb, Ian J. S.
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p. 3979 - 3985
(2021/02/03)
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- Metal-Free Geminal Difunctionalization of Diazocarbonyl Compounds: A One-Pot Multicomponent Strategy for the Construction of α,β-Diamino Carbonyl Derivatives
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An unprecedented three-component domino oxidative coupling of diazocompounds for the efficient synthesis of α-azido-β-amino esters with non-activated dimethylamino compounds and simple TMSN3 was achieved. The main features of this method include metal-free catalysis, satisfactory functional group tolerance, general applicability in complex molecule architectures, and excellent diastereoselectivity in the presence of chiral auxiliaries. In addition, several related control experiments have been conducted to investigate the reaction mechanism.
- Zhu, Dan,Yao, Yuan,Zhao, Rong,Liu, Yang,Shi, Lei
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p. 4805 - 4809
(2018/03/21)
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- STEROID-HORMONE CONJUGATES WITH POLYAMINES AND THEIR THERAPEUTIC USE AS ANTI-CANCER AND ANGIOSTATIC AGENTS
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Compounds of formula (I): {in which: one of R1 and R2 represents a group of formula (II): -NH-(CH2)N-NH-[(CH2)m-NH]x-[(CH2)p-NH]y (II) [where n, m and p each represents a number from 2 to 6; and x and y each represents zero or a number from 1 to 2]; and the other of R1 and R2 represents hydrogen, oxo, hydroxyl, a Cl - C6 alkanoyl group or said group of formula (II); R3 and R4 each represents oxo, hydroxy, mercapto, hydrogen, halogen, alkoxy or aryloxy; R5 represents hydrogen or methyl or is not present; the dotted line indicates a single or douse bond; and the dotted circle indicates none, one, two or three double bonds between pairs of adjacent carbon atoms}; and esters thereof are useful for the treatment or prevention of tumours and/or diabetic retinopathy.
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Page/Page column 37
(2008/06/13)
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- TOPICAL ANTIANDROGENIC STEROIDS
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Steroidal antiandrogens and pharmaceutical compositions thereof, are used for reduction of the risk of developing, or for treatment of, androgen-dependent skin related diseases. In preferred embodiments, the antiandrogen EM-3180 is used for reduction of t
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- An efficient synthesis of novel estrieno[2.3-b] and [3.4-c]pyrroles
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An efficient protocol for the preparation of novel estrieno[2.3-b] and [3.4-c]pyrroles 1 and 2 using Pd(0)-catalyzed amination and Bischler indole synthesis is described.
- Zhang, Xuqing,Sui, Zhihua
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p. 3071 - 3073
(2007/10/03)
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- New efficient pathway for the synthesis of 3-aminoestrone
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3-Aminoestrone, a non-natural C-18 steroid, was synthesized by the classical and by a new efficient pathway, the latter using benzophenone imine as an ammonia equivalent in the palladium(0)-catalysed amination of estrone-triflate. This methodology circumv
- Radu, Ioan-Iosif,Poirier, Donald,Provencher, Louis
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p. 7617 - 7619
(2007/10/03)
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