36969-89-8Relevant articles and documents
Of the trometamol prostaglandin F2 α synthesis method (by machine translation)
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, (2017/08/30)
The invention discloses a of the trometamol prostaglandin F2 α synthesis method, as the compound (-) - Corey lactone diol as raw materials, through the oxidation reaction to obtain lactone aldehyde, lactone aldehydechain after the weidiWeidi Greecehuo Naer reaction with - the lower side of the splicing an olefin, the olefin double-carbonyl after reduction to obtain the alcohol, with puncture ylide - wittich reaction the upper side of the obtained prostaglandin F2 α, then the prostaglandin F2 α of the trometamol after crystallization by dissolving of the trometamol prostaglandin F2 α. The synthesis method, without noble metal catalyst, there is little side reaction, high yield, low cost, less pollution, is suitable for industrial production. (by machine translation)
PROCESS FOR THE PREPARATION OF TREPROSTINIL
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Page/Page column 48; 49, (2016/05/02)
The invention provides a new process for the preparation of treprostinil of formula (I) and its salts using several new intermediates during the building of the ringsystem.
A facile route for synthesis of (±)-dinoprost, (±)-carboprost and its analogs
Shankar,Mohan, H. Rama,Prasad, U. Viplava,Krishna, M. Hari,Rao, P. Mareswar,Lakshmikumar,Subbaraju, Gottumukkala V.
, p. 913 - 920 (2013/06/04)
A general synthetic approach was developed for (±)-dinoprost (1), (±)-carboprost (2) and their analogs (3-5) through a key intermediate (6). Compound 6 can be converted into the target compounds in two or three steps. Diastereomeric separation was accomplished easily for obtaining (±) dinoprost. Separation of diastereomers was difficult for (±) carboprost and their analogs. Key intermediate 6 was obtained, in turn, from (±)-corey lactone.
Efficient synthesis of α,β-unsaturated alkylimines performed with allyl cations and azides: Application to the synthesis of an ant venom alkaloid
Hayashi, Kyohei,Tanimoto, Hiroki,Zhang, Huan,Morimoto, Tsumoru,Nishiyama, Yasuhiro,Kakiuchi, Kiyomi
supporting information, p. 5728 - 5731 (2013/01/15)
An efficient synthesis of α,β-unsaturated alkylimines at low temperature using azides has been developed. Carbocations generated from allyl alcohols helped achieve a rapid conversion under mild conditions with azides to afford reactive α,β-unsaturated imines. Hydroxy or alkoxy groups are essential for these transformations, and utilizing readily accessible allyl alcohols gave a wide extension of substrates. The efficiency of this novel method is demonstrated in the total synthesis of an iminium ant venom alkaloid.
Discovery of a novel EP2/EP4 dual agonist with high subtype-selectivity
Kambe, Tohru,Maruyama, Toru,Nakano, Masayuki,Nakai, Yoshihiko,Yoshida, Tadahiro,Matsunaga, Naoki,Oida, Hiroji,Konaka, Akira,Maruyama, Takayuki,Nakai, Hisao,Toda, Masaaki
scheme or table, p. 396 - 401 (2012/02/16)
A series of γ-lactam prostaglandin E1 analogs bearing a 16-phenyl moiety in the ω-chain and aryl moiety in the α-chain were synthesized and biologically evaluated. Among the tested compounds, γ-lactam PGE analog 3 designed as a structural hybrid of 1 and 2 was discovered as the most optimized EP2/EP4 dual agonist with excellent subtype-selectivity (Ki values: mEP2 = 9.3 nM, mEP4 = 0.41 nM). A structure-activity relationship study is presented.
On a safe and practical method for the preparation of β-keto phosphonates
Corbel, Bernard,L'Hostis-Kervella, Isabelle,Haelters, Jean-Pierre
, p. 2561 - 2568 (2007/10/03)
Acylations of the magnesium enolate derivatives of trimethyl and triethylphosphonoacetates, using a magnesium chloride-triethylamine system, lead to 2-acetylphosphonoacetates which are decarbalkoxylated to give β-keto phosphonates.
Copper(II) Bromide Utilization in the Synthesis of 15-Keto-PGB1 and its 16,16-Dimethyl Analog
Martin, I.,Anvelt, J.,Valimae, T.,Pehk, T.,Lille, O.
, p. 2597 - 2605 (2007/10/02)
Title compounds, monomeric intermediates of biologically active prostaglandin oligomers were synthesized using cupric bromide for introduction of a double bond into the prostanoid cyclopentane ring.
10-Hydroxy PGC compounds
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, (2008/06/13)
10α-Hydroxy-11-desoxy-prostaglandin analogs of the PGE1 and PGE2 and PGF1α and PGF2α series, the 11-dehydro derivatives thereof as well as the 9,10-ketals in the PGF series, and methods of preparing same, 9-keto-10α,15α-dihydroxyprosta-13-trans-enoic or 5-cis,13-trans-dienoic acid, 9α,10α,15α-trihydroxyprosta-11,13-trans-dienoic or 5-cis, 11,13-trans-trienoic acid and 9α,10α-isopropyli-denedioxy-15α-hydroxyprosta-13-trans-enoic or 5-cis,13-trans-dienoic acid are representative of the class. Also included are the corresponding pharmaceutically acceptable, non-toxic esters, ethers and salts. These compounds possess prostaglandin-like activity and thus are useful in the treatment of mammals, where prostaglandins are indicated.
Polyunsaturated prostaglandin derivatives
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, (2008/06/13)
Novel prostaglandin dehydro analogs of the PGA and PGB series and the 9-hydroxy-derivatives thereof, which possess a diethylenic unsaturation in the carboxylic acid chain and may be additionally substituted at C-4, C-6, C-9 and/or C-15 by a methyl, ethyl or propyl group, as well as the C-20-nor, bisnor or C-20 alkyl derivatives thereof, the alkyl group being of a straight chain and containing from 1 to 5 carbon atoms inclusive,, and processes for making same. 9-keto-15α-hydroxyprosta-4,5,10,13-trans-tetraenoic acid and 9-keto-15α-hydroxyprosta-4,5,8(12),13-trans-tetraenoic acid are representative of the class. Also included are the pharmaceutically acceptable, non toxic esters and salts of the carboxylic acid function and the pharmaceutically acceptable, non toxic esters and/or ethers of the secondary hydroxyl groups. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals, where prostaglandins are indicated.
