- Halogenolysis of Benzylcobaloximes
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The reaction of substituted benzylcobaloximes p-RC6H4Co(dmgH)2-Py (R=OMe, NHCOCH3 and NMe2) and m-RC6H4CH2Co(dmgH)2Py (R=Me, OMe) with halogens (Cl2 and Br2) in chloroform under nitrogen forms ring substituted organic and organometallic products.
- Gupta, B. D.,Kumar, Manoj
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Read Online
- Structural studies of biarylpyridines fluorophores lead to the identification of promising long wavelength emitters for use in fluorescent chemosensors
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Fluorescent chemosensors - molecules whose fluorescence emission changes in response to a reversible binding event - require both a substrate binding domain and a reporting fluorophore. Our approach to chemosensor development is based on a combination of a new signaling mechanism and a modular fluorophore synthesis. The latter feature has facilitated detailed study of the properties of polyarylpyridine fluorophores, and has led to the identification of a visibly-emissive pyridine as a promising lead structure for chemosensor development. The results of this study are described herein.
- Fang,Mello,Finney
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Read Online
- Regiocontrolled and Stereoselective Syntheses of Tetrahydrophthalazine Derivatives using Radical Cyclizations
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Tetrahydrophthalazine derivatives have found important applications in pharmaceutical research, but existing synthetic methods are unable to access them regio- and stereoselectively. Here, a new approach is presented that addresses these challenges by utilizing a 6-endo-trig radical cyclization in the key step. The desired tetrahydrophthalazines can be accessed in high yields (55–98 %) and high diastereoselectivities for the trans-product (>95:5) starting either from readily accessible hydrazones, or from the corresponding aldehydes and substituted Boc-hydrazides in a one-pot process. The synthetic versatility of the tetrahydrophthalazine core was demonstrated by its straightforward conversion to dihydro-phthalazines, phthalazines, or pyrazolo dione derivatives. Furthermore, the N?N bond was reduced to afford a new route to 1,4-diamines.
- Zhang, Wei,Mo, Jia Yi,He, Weiying,Kennepohl, Pierre,Sammis, Glenn M.
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supporting information
p. 976 - 980
(2019/01/04)
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- Stereoselective Convergent Synthesis of Tetrahydro-5 H-benzo[c]fluorene via Nine-Membered Ring-Closing Metathesis and Transannular Acid-Mediated Cyclization/Nucleophilic Addition
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The diene methyl ethers or acetates, constructed from the Li-Br exchange/addition reactions of 2-vinylbenzaldehydes and 2-(but-3-en-1-yl)bromoarenes followed by etherification or acetylation of the corresponding alcohols, smoothly underwent the ring-closi
- Lekky, Anek,Ruengsatra, Tanachote,Ruchirawat, Somsak,Ploypradith, Poonsakdi
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p. 5277 - 5291
(2019/05/10)
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- STEREORETENTIVE CROSS-COUPLING OF BORONIC ACIDS
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The present disclosure provides tri-orthoalkylphenyl phosphine catalysts that are tuned electrically and sterically. Method of using the catalyst for cross-coupling of unactivated secondary boronic acids with near-perfect levels of site- and stereoretention are also provided.
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Paragraph 0112; 0186-0188
(2018/11/21)
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- CATALYSTS
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A catalyst comprising (i) an asymmetric complex of formula (I) wherein M is zirconium or hafnium; each X is a sigma ligand; L is a divalent bridge selected from —R′2C—, —R′2C—CR′2—, —R′2Si—, —R′2Si—SiR′2—, —R′2Ge—, wherein each R′ is independently a hydrogen atom, C1-C20-alkyl, tri(C1-C20-alkyl)silyl, C6-C20-aryl, C7-C20-arylalkyl or C7-C20-alkylaryl; R2 and R2′ are each independently linear C1-10 hydrocarbyl; R5 and R5′ are each independently hydrogen or a C1-20 hydrocarbyl group; R6 and R6′ are each independently hydrogen or a C1-20 hydrocarbyl group; R7 is hydrogen or a C1-20 hydrocarbyl group or is ZR3; Z is O or S, preferably O; R3 is a C1-10 hydrocarbyl group; Ar is an aryl or heteroaryl group having up to 20 carbon atoms optionally substituted by one or more groups R8; Ar′ is an aryl or heteroaryl group having up to 20 carbon atoms optionally substituted by one or more groups R8′; and R8 and R8′ are each independently is a C1-20 hydrocarbyl group; with the proviso that at least one of R6 or R7 is not H; and (ii) a cocatalyst comprising a compound of a group 13 metal, e.g. boron.
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- Rhodium-Catalyzed, Enantioselective Hydroacylation of ortho-Allylbenzaldehydes
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The development of a rhodium catalyst for endo- and enantioselective hydroacylation of ortho-allylbenzaldehydes is reported. A catalyst generated in situ from [Rh(COD)Cl]2, (R)-DTBM-SEGPHOS, and NaBARF promotes the desired hydroacylation reactions and minimizes the formation of byproducts from competitive alkene isomerization and ene/dehydration pathways. These rhodium-catalyzed processes generate the 3,4-dihydronaphthalen-1(2H)-one products in moderate-to-high yields (49-91%) with excellent enantioselectivities (96-99% ee).
- Johnson, Kirsten F.,Schmidt, Adam C.,Stanley, Levi M.
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supporting information
p. 4654 - 4657
(2015/10/12)
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- Catalyst
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A catalyst comprising (i) an asymmetric complex of formula (I) wherein M is zirconium or hafnium; each X is a sigma ligand; L is a divalent bridge selected from -R'2C-, -R'2C-CR'2-, -R'2Si-, -R'2Si-SiR'2-, -R'2Ge-, wherein each R' is independently a hydrogen atom, C1-C20-alkyl, tri(C1-C20-alkyl)silyl, C6-C20-aryl, C7-C20-arylalkyl or C7-C20-alkylaryl; R2 and R2' are each independently linear C1-10 hydrocarbyl; R5 and R5' are each independently hydrogen or a C 1-20 hydrocarbyl group; R6 and R6' are each independently hydrogen or a C1-20 hydrocarbyl group; R7 is hydrogen or a C1-20 hydrocarbyl group or is ZR3; Z is O or S, preferably O; R3 is a C1-10 hydrocarbyl group; Ar is an aryl or heteroaryl group having up to 20 carbon atoms optionally substituted by one or more groups R8; Ar' is an aryl or heteroaryl group having up to 20 carbon atoms optionally substituted by one or more groups R8'; R8 and R8' are each independently is a C1-20 hydrocarbyl group; with the proviso that at least one of R6 or R7 is not H; and (ii) a cocatalyst comprising a compound of a group 13 metal, e.g. boron.
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Page/Page column
(2014/07/08)
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- A route to the 9,10-secosteroid astrogorgiadiol featuring a key sp 2-sp3 Suzuki type cross-coupling
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The described semi-synthetic route differs from the previously published approaches by an original C-7-C-8 disconnection. The kinetic enol triflate of Grundmann ketone was chosen as the CD-ring platform on which to couple an A-ring synthon via a challengi
- Médard, Guillaume
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p. 186 - 196
(2014/01/06)
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- Synthesis of methoxy-substituted picenes: Substitution position effect on their electronic and single-crystal structures
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A series of picenes having methoxy groups was synthesized through Pd-catalyzed Suzuki-Miyaura couplings or Wittig reaction/intramolecular cyclization sequences, and their physicochemical properties and single-crystal structures were evaluated. The substit
- Mori, Hiroki,Chen, Xi-Chao,Chang, Ning-Hui,Hamao, Shino,Kubozono, Yoshihiro,Nakajima, Kiyohiko,Nishihara, Yasushi
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p. 4973 - 4983
(2014/06/23)
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- CATALYSTS
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A racemic complex of formula (I), wherein ? M is zirconium or hafnium; ? each X is a sigma ligand; ? L is a divalent bridge selected from -R'2C-, -R'2C-CR'2, -R'2Si-, - R'2Si-SiR'2-, -R'2Ge-, wherein each R' is independently a hydrogen atom, C1-20-hydrocarbyl, tri(C1-20-alkyl)silyl, C6-20-aryl, C7-20-ary- lalkyl or C7-20-alkylaryl; ? R2 and R2' are each independently a C1-20 hydrocarbyl radical optionally containing one or more heteroatoms from groups 14-16; ? R5' is a C1-20 hydrocarbyl group optionally containing one or more heteroatoms from groups 14-16 and optionally substituted by one or more halo atoms.
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Page/Page column 78; 79
(2013/03/26)
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- Substituent effects on oxidation-induced formation of quinone methides from arylboronic ester precursors
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A series of arylboronic esters containing different aromatic substituents and various benzylic leaving groups (Br or N+Me3Br -) have been synthesized. The substituent effects on their reactivity with H2O2 and formation of quinone methide (QM) have been investigated. NMR spectroscopy and ethyl vinyl ether (EVE) trapping experiments were used to determine the reaction mechanism and QM formation, respectively. QMs were not generated during oxidative cleavage of the boronic esters but by subsequent transformation of the phenol products under physiological conditions. The oxidative deboronation is facilitated by electron-withdrawing substituents, such as aromatic F, NO2, or benzylic N+Me 3Br-, whereas electron-donating substituents or a better leaving group favor QM generation. Compounds containing an aromatic CH 3 or OMe group, or a good leaving group (Br), efficiently generate QMs under physiological conditions. Finally, a quantitative relationship between the structure and activity has been established for the arylboronic esters by using a Hammett plot. The reactivity of the arylboronic acids/esters and the inhibition or facilitation of QM formation can now be predictably adjusted. This adjustment is important as some applications may benefit and others may be limited by QM generation. Tunable quinone methide formation: Aromatic substituents and the benzylic leaving group strongly affect the H 2O2-induced formation of quinone methides (QMs) from arylboronic esters (see scheme). The reactivity of arylboronic esters can be predictably adjusted by varying substituents. Copyright
- Cao, Sheng,Christiansen, Robin,Peng, Xiaohua
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p. 9050 - 9058
(2013/07/26)
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- Atropoisomeric (P,N) ligands for the highly enantioselective Pd-catalyzed intramolecular asymmetric α-arylation of α-branched aldehydes
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Three-in-one: A short synthetic route readily gives access to a new class of chiral (P,N) ligands characterized by three distinct elements of chirality. These ligands are highly enantioselective in the challenging Pd-catalyzed intramolecular asymmetric α-
- Nareddy, Pradeep,Mantilli, Luca,Guenee, Laure,Mazet, Clement
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supporting information; scheme or table
p. 3826 - 3831
(2012/06/01)
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- Palladium-catalyzed intramolecular decarboxylative coupling of arene carboxylic acids/esters with aryl bromides
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Give me a ring? An efficient approach has been developed for the intramolecular decarboxylative coupling of arene carboxylic acids/esters with aryl bromides catalyzed by palladium (see scheme). From a synthetic viewpoint, this method is highly attractive because the catalyst loading is low, the optimized reaction conditions are mild, and the substrate scope is broad. Copyright
- Shen, Zengming,Ni, Zhenjie,Mo, Song,Wang, Jing,Zhu, Yamin
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supporting information; experimental part
p. 4859 - 4865
(2012/06/04)
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- Total synthesis of cortistatins A and J
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This paper describes the details of our synthetic studies on the marine steroidal alkaloids cortistatins A and J. The key features of our strategy include (i) an efficient Knoevenagel/electrocyclic strategy to couple the diketone and the CD-ring fragment, (ii) a chemoselective radical cyclization to construct the oxabicyclo[3.2.1]octene B-ring system, (iii) a highly stereocontrolled installation of the isoquinoline unit, and (iv) a late-stage functionalization of the A-ring.
- Yamashita, Shuji,Iso, Kentaro,Kitajima, Kazuki,Himuro, Masafumi,Hirama, Masahiro
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experimental part
p. 2408 - 2425
(2011/06/20)
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- Synthesis of benzo- and naphtho-fused bicyclo[n.3.1]alkane frameworks with a bridgehead nitrogen function by palladium-catalyzed intramolecular α′-arylation of α-nitroketones
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The C-alkylation of cyclic α-nitroketones with α-halobenzyl halides in the presence of DBU followed by a Pd-catalyzed intramolecular C-arylation afforded benzo-and naphtho-fused bicyclo[n.3.1]alkane derivatives (n = 3, 4, 5) in excellent overall yields for the two-step sequence. In some of the reactions starting from α-nitrocyclooctanone, the major products were fused indane derivatives arising from an intramolecular attack of an intermediate Pd species onto the carbonyl group, followed by elimination.
- Giorgi, Giorgio,Maiti, Swarupananda,Lopez-Alvarado, Pilar,Menendez, J. Carlos
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supporting information; experimental part
p. 2722 - 2730
(2011/05/12)
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- Synthesis of N-alkoxyindol-2-ones by copper-catalyzed intramolecular N-arylation of hydroxamates
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The first example of copper-catalyzed intramolecular N-arylation of hydroxamic acid derivatives is presented. Based on this transformation a new method for the synthesis of N-alkoxyindol-2-ones from 2-(2-bromoaryl) acetylhydroxamates has been developed. T
- Kukosha, Tatyana,Trufilkina, Nadezhda,Katkevics, Martins
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supporting information; experimental part
p. 2525 - 2528
(2011/11/13)
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- An ortho-quinodimethane route to Lasofoxifene and U23469
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Lasofoxifene, a third-generation selective estrogen receptor modulator, could be synthesized via regio-and stereoselective [4 + 2] cycloaddition between an ortho-quinodimethane and a borylalkene. This protocol was also applicable to the synthesis of antie
- Yoshida, Hiroto,Yoshida, Ryuma,Mukae, Masashi,Ohshita, Joji,Takaki, Ken
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supporting information
p. 1272 - 1274
(2015/09/22)
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- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
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Page/Page column 176-177
(2011/04/14)
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- Efficient discovery of fluorescent chemosensors based on a biarylpyridine scaffold
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(Figure Presented) The discovery of several fluorescent chemosensors for Hg(II) and Ag(I) In mixed aqueous solution Is reported. The ease with which these fluorlonophores were prepared from a common core underscores the utility of conformational restriction as a signaling mechanism. In addition, for the first time, significant changes were observed In biarylpyridlne emission wavelength, allowing ratlometric detection of Hg(II) and Ag(I). Finally, on the basis of computational analyses, beneficial structural modifications were predicted for the next generation of chemosensors.
- Malashikhin, Sergey A.,Baldridge, Kim K.,Finney, Nathaniel S.
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supporting information; scheme or table
p. 940 - 943
(2010/06/16)
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- Syntheses of macrocyclic bis(bibenzyl) compounds derived from perrottetin e
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Macrocyclic bis(bibenzyl) compounds are natural products from liverworts and are of growing interest due to recent reports on new isolated compounds and on their remarkable biological activities. We report here on a flexible and general approach to the to
- Speicher, Andreas,Groh, Matthias,Hennrich, Markus,Huynh, Anh-Minh
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experimental part
p. 6760 - 6778
(2011/03/18)
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- A synthesis-driven structure revision of 'plagiochin E', a highly bioactive bisbibenzyl
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Recently, a bisbibenzyl named plagiochin E showing remarkable antifungal and antitumor activities was isolated from Marchantia polymorpha, a liverwort. The total synthesis of the proposed structure for plagiochin E and of two structurally and biosynthetic
- Speicher, Andreas,Groh, Matthias,Zapp, Josef,Schauml?ffel, Anu,Knauer, Michael,Bringmann, Gerhard
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scheme or table
p. 1852 - 1858
(2009/12/05)
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- N-(5-fluoro-2-phenoxyphenyl)-N-(2-[131I]iodo-5-methoxybenzyl) acetamide: A potent iodinated radioligand for the peripheral-type benzodiazepine receptor in brain
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To image the peripheral-type benzodiazepine receptor (PBR) in vivo, we previously developed two positron emission tomography (PET) ligands, N-(2-[ 11C],5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide ([ 11C]1a) and its [sup
- Zhang, Ming-Rong,Kumata, Katsushi,Maeda, Jun,Haradahira, Terushi,Noguchi, Junko,Suhara, Tetsuya,Halldin, Christer,Suzuki, Kazutoshi
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p. 848 - 855
(2007/10/03)
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- Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: Structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109
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Following the discovery of a new series of benzimidazole derivatives bearing a diarylmethyl group as inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase (HCV NS5B RdRp), we extended the structure-activity relationship (SAR) study to analogue
- Hirashima, Shintaro,Suzuki, Takayoshi,Ishida, Tomio,Noji, Satoru,Yata, Shinji,Ando, Izuru,Komatsu, Masakazu,Ikeda, Satoru,Hashimoto, Hiromasa
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p. 4721 - 4736
(2007/10/03)
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- Reversing the discovery paradigm: A new approach to the combinatorial discovery of fluorescent chemosensors
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We report here a new approach to the discovery of fluorescent chemosensors in which a new signaling mechanism allows a core fluorophore to be used in a combinatorial search for new binding events, thus reversing the reigning discovery paradigm. Copyright
- Mello, Jesse V.,Finney, Nathaniel S.
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p. 10124 - 10125
(2007/10/03)
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- SEROTONINE REUPTAKE INHIBITOR
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There is provided a selective serotonin reuptake inhibitor having affinity for serotonin 1A receptors which comprises a cyclic amine represented by the formula: wherein G represents a formula (2): a prodrug of said cyclic amine, or a pharmaceutically acceptable salt of said cyclic amine or prodrug, as an active ingredient.
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- Efficient synthesis of isoplagiochin D, a macrocyclic bis(bibenzyls), by utilizing an intramolecular Suzuki-Miyaura reaction
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Isoplagiochin D, a highly strained macrocyclic bis(bibenzyls) isolated from the liverwort Pladiochila fruticosa, was synthesized in 10.6% overall yield for the 11 steps by using Horner-Wadsworth-Emmons and Suzuki-Miyaura protocols. Isoplagiochin D, a highly strained macrocyclic bis(bibenzyls) with two biaryl units isolated from the liverwort Pladiochila fruticosa, was prepared in 10.6% overall yield for the 11 steps by an efficient synthetic approach involving the construction of two bibenzyl and one biaryl units using Horner-Wadsworth-Emmons and Suzuki-Miyaura protocols.
- Esumi, Tomoyuki,Wada, Mitsumasa,Mizushima, Eri,Sato, Norimasa,Kodama, Mitsuaki,Asakawa, Yoshinori,Fukuyama, Yoshiyasu
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p. 6941 - 6945
(2007/10/03)
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- SUBSTITUTED AMINO PHENYLACETIC ACIDS, DERIVATIVES THEREOF, THEIR PREPARATION AND THEIR USE AS CYCLOOXYGENASE 2 (COX-2) INHIBITORS
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Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3-C8)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3-C6)cycloalkylmonocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.
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- Serotonin reuptake inhibitor
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A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient: wherein R0 is a hydrogen atom, a halogen atom, an alkyl group, a substituted alkyl group, a hydroxyl group, an alkoxy group or the like, R3 is a hydrogen atom or the like, Y is an alkylene group or the like, Z is a hydrogen atom, a cycloalkyl group, an aryl group or the like, n is 1, 2 or 3, and m is 2, 3, 4, 5 or 6.
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- Synthesis of 3-hexahelicenol and its transformation to 3-hexahelicenylamines, diphenylphosphine, methyl carboxylate, and dimethylthiocarbamate
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A nonphotochemical synthetic route to 3-hexahelicenol is reported. It involves a key [2+2+2] cycloisomerization of CH3O-substituted triyne that is readily available from 1-methoxy-3-methylbenzene and 1-bromo-2-(bromomethyl)naphthalene. Further
- Teply, Filip,Stara, Irena G.,Stary, Ivo,Kollarovic, Adrian,Saman, David,Vyskocil, Stepan,Fiedler, Pavel
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p. 5193 - 5197
(2007/10/03)
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- Vitronectin receptor antagonists
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Compounds having a benzodiazepinyl core structure are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis, angiogenesis, tumor growth and metastasis, atherosclerosis, restenosis and inflammation.
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- Asymmetric conjugate addition reaction
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This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.
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Page column 26
(2010/01/30)
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- Method for stimulating bone formation
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A method for stimulating bone formation by administering integrin binding compounds which cause the release of osteocalcin from osteoblasts is disclosed.
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- Intramolecular homolytic substitution at selenium: Synthesis of novel selenium-containing vitamin E analogues
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Treatment of 1-(benzylselenenyl)-5-butyl-5-nonanol (10) with oxalyl chloride followed by the sodium salt of N-hydroxypyridine-2-thione afforded the corresponding pyridine-2-thione-N-oxycarbonyl (PTOC) oxalate ester which was not isolated but immediately heated to provide 2,2-dibutylselenane (7). This transformation presumably involves a tertiary alkyl radical that undergoes intramolecular homolytic substitution at selenium with loss of the benzyl radical to provide the selenium-containing ring system (7). A similar protocol, when applied to 1-(2-benzylselenenyl-5-methoxyphenyl)-3-methyl3-heptanol (18) and 1-(2-benzylselenenyl-5-methoxyphenyl)-3,7,11,15-tetramethyl-3-hexadecanol (19), followed by deprotection, afforded the selenium-containing α-tocopherol analogues 4 and 1f, respectively, in moderate yields. To the best of our knowledge, these transformations represent the first examples of tertiary radicals involved in homolytic substitution chemistry at selenium.
- Al-Maharik,Engman,Malmstroem,Schiesser
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p. 6286 - 6290
(2007/10/03)
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- Intermediates in a process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine
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This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (-)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.
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- Total syntheses of plagiochins A and D, macrocyclic bis(bibenzyls), by Pd(0) catalyzed intramolecular Stille-Kelly reaction
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Total syntheses of plagiochins A (1) and D (4), the former of which exhibits a significant neurotrophic activity, have been accomplished. The key 16-membered ring closure in 4 has been achieved directly from the dibromoperrottetin derivative (7) by Pd(0)
- Fukuyama, Yoshiyasu,Yaso, Hideyuki,Mori, Takashi,Takahashi, Hironobu,Minami, Hiroyuki,Kodama, Mitsuaki
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p. 259 - 274
(2007/10/03)
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- Synthesis of (-)-astrogorgiadiol
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Reaction of Rh2(S)-PTPA4 with the (R)-citronellol-derived α-diazo-β-ketoester 1 led to the formation of cyclic β-ketoester 2 in 95% yield and 48% diastereomeric excess. The purity of 2 was increased to >99% de after one crystallization. To demonstrate its utility in steroid total synthesis, the β-ketoester 2 was carried on to secosteroid (-)-astrogorgiadiol (3), a naturally occuring vitamin D analogue with antiproliferative properties.
- Taber,Malcolm
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p. 944 - 953
(2007/10/03)
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- Vitronectin receptor antagonist
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A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.
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- Chemical and in vitro syntheses of brominated and chlorinated 3,4′-dihydroxybibenzyls (halogenated lunularins)
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Ten halogenated lunularins 16, 17, 26, 27, 30, 31, 36, 37, 42 and 43 as model substances for a new class of halometabolites isolated from bryophytes are prepared by chemical total syntheses according to a Wittig-protocol using halogenated aldehydes and ph
- Speicher, Andreas
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p. 162 - 168
(2007/10/03)
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- Total synthesis of plagiochin D, a macrocyclic bis(bibenzyl) from liverworts by intramolecular Still-Kelly reaction
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Plagiochin D (4), a unique macrocyclic bis(bibenzyl) having both a biphenyl ether and a biaryl units isolated from the liverwort Plagiochila acanthophylla, was synthesized. The key 16-membered ring closure of a dibromoperrottetin. A derivative 13 was realized by Pd(0) catalyzed intramolecular Still-Kelly reaction.
- Fukuyama, Yoshiyasu,Yaso, Hideyuki,Nakamura, Kazuhiko,Kodama, Mitsuaki
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p. 105 - 108
(2007/10/03)
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- Aminotetralin derivative and compositions and method of use thereof
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The invention relates to aminotetralin derivatives of the formula I: STR1 wherein: R1 is methyl or ethyl; R2 is hydrogen, halogen, lower-alkoxy or thiolower-alkyl; R3 is hydrogen, halogen, lower-alkoxy or lower-alkyl; and
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- Regioselective aryl radical cyclisation. Part 2. Synthesis of octahydro-1H-dibenzo[a,d]cycloheptenes through 7-endo ring closure
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A simple convergent synthesis of trans- and cis-octahydro-1H-dibenzo[a,d]cycloheptenes 15a-c and 16a-c and 20a-c and 21a-c through implementation of a regioselective 7-endo-trig-aryl radical cyclisation of the respective 2-(o-bromoarylethyl)-1-methylenecy
- Ghosh, Ajit K.,Mukhopadhyaya, Jayanta K.,Ghatak, Usha Ranjan
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p. 2747 - 2755
(2007/10/03)
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- AN IMPROVED SYNTHESIS OF 7-METHOXYISOCHROMAN-3-ONE: A SYNTHON FOR GENERATION OF o-QUINODIMETHANES
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7-Methoxyisochroman-3-one (8) has been synthesized from 2-bromo-5-methoxybenzyl methyl ether (3) in overall high yield.
- Kanapure, S. P.,Das, K. G.,Bhawal, B. M.
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p. 1205 - 1212
(2007/10/02)
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