74-41-9Relevant articles and documents
Mustard Carbonate Analogues as Sustainable Reagents for the Aminoalkylation of Phenols
Annatelli, Mattia,Trapasso, Giacomo,Salaris, Claudio,Salata, Cristiano,Castellano, Sabrina,Aricò, Fabio
supporting information, p. 3459 - 3464 (2021/05/24)
N,N-dialkyl ethylamine moiety can be found in numerous scaffolds of macromolecules, catalysts, and especially pharmaceuticals. Common synthetic procedures for its incorporation in a substrate relies on the use of a nitrogen mustard gas or on multistep syntheses featuring chlorine hazardous/toxic chemistry. Reported herein is a one-pot synthetic approach for the easy introduction of aminoalkyl chain into different phenolic substrates through dialkyl carbonate (β-aminocarbonate) chemistry. This new direct alcohol substitution avoids the use of chlorine chemistry, and it is efficient on numerous pharmacophore scaffolds with good to quantitative yield. The cytotoxicity via MTT of the β-aminocarbonate, key intermediate of this synthetic approach, was also evaluated and compared with its alcohol precursor.
Synthesis of tetracyclic heterocompounds as selective estrogen receptor modulators. Part 2. Process improvement for scale-up of 2,5,8-substituted 11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohepta-[1,2-a]naphthalene derivatives
Li, Xun,Reuman, Michael,Russell, Ronald K.,Youells, Scott,Beish, Sandra,Hu, Zhiyong,Branum, Shawn,Jain, Nareshkumar,Sui, Zhihua
, p. 731 - 738 (2012/12/29)
An improved, reproducible nonchromatographic process for scale-up synthesis of 2,5,8-substituted 11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohepta[1,2-a] naphthalene derivatives as selective estrogen receptor modulators (SERMs) is described. The titled comp
Aminoindazole derivatives
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, (2008/06/13)
A compound of the formula (I): STR1 wherein W1 and W2 each independently is a hydrogen atom or a STR2 group wherein Y is a n-C1-6 alkylene group or a n-C1-6 alkylene group having a C1-6 alkyl group substituent; and R1 and R2 each independently is a hydrogen atom or a C1-6 alkyl group, and STR3 group in STR4 group may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C1-4 alkyl group, hydroxyl group or halogen atom as a substituent; Z1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C1-3 alkyl group or a methoxy group; Z2 is a hydrogen atom or an amino group; when W1 and W2 are both hydrogen atoms, Z1 is a hydroxyl group or an iodine atom and Z2 is hydrogen atom, or Z1 and Z2 are both amino groups; when Z1 and Z2 are both hydrogen atoms, the STR5 group in either W1 or W2 is a morpholino group; when Z1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z2 is a hydrogen atom; when Z1 is an amino group, Z2 is a hydrogen atom or an amino group; when Z1 is a methyl group, a methoxy group or an amino group, Z1 is in the 5-position; when Z1 is an iodine atom, Z1 is in the 5- or 7-position; and when Z1 and Z2 are both amino groups, Z1 and Z2 are in the 5- and 7-positions; and the physiologically acceptable acid addition salt thereof which compounds have pharmaceutical utility, e.g.: treating inflammation.
