Decarboxylative oxidation of lithocholic acid

Summary:

A new series of bile acid-based trioxanes have been synthesized and assessed for their antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice by oral route.

The Reaction of Interest:

Decarboxylative oxidation of...

Novel and less expensive Hypo-SiF synthesis

• Hypo-SiF is uniquely new in finding the high concentration of HOCl
• Hypo-SiF is reported to be good in finding the HOCl concentration and pH of the media simultaneously at lower concentrtion
• To obtain clear results, Hypo-SiF needs to be improved and...

Hydrostannation of Terminal Acetylenes

The hydrostannation of alkynes is frequently used for the synthesis of vinyl stannanes, which can be subjected to further modifications via a Stille coupling. The major drawbacks of this process result from the difficulties which arise in the control of the...

Seminal paper for phase-transfer Heck-Mizoroki cross coupling

A pinacle reaction of the synthesis required the cross coupling off a two highly heteroatom functionalised fragments, the use of traditional Heck conditions, such as palladium (II) acetate, triphenyl phosphine and triethylamine afforded poor yields and...

Reproducible on smaller scale

Synthesized 2-[N-( tert -Butoxycarbonyl)amino]thiophene (25) and a similar compound (2-[N-( tert -Butoxycarbonyl)amino]-5-bromothiophene) following the same procedure described in the article as method F.

For the synthesis of 25, the reaction was scaled...

Orthosilicate-Mediated Esterification of Monosubstituted Phosphinic Acids

The methodology developed by Montchamp and co-workers demonstrated a mild and reliable way to esterify the monosubstituted phosphinic acids.

I repeated the preparation of substrate 3 as the entry 5 in table 1 followed their protocol.  The reaction...

reproducible process and yield

Synthesized similar structures to (13)- "4'-bromo-2',3,5,6'-tetramethoxy-[1,1'-biphenyl]-4-yl trifluoromethanesulfonate" and also other subtitude functional group on 2',3,5,6' position- using the same procedures as are written in the paper in Supporting...

Blocking diazonium couplings of aromatic rings

H. Kondo and E. Ochiai Ann. Chem. 1929 470 p224 reported using the iodo group to block Pschorr diazonium cyclizations into an aromatic carbon position when making polycyclic aromatics.  This protocol was repeated by K. Goto and H. Sudzuki Bull. Chem. Soc. Jpn...

Review of the novel materials for future organic electronics

The manuscript entitled ''A cyclic triphenylamine dimer for organic field-effect transistors with high performance'' is a nice piece of work. A new OFET based on triphenylamine units with a macrocyclic architect has been described with its potential use as...

Good synthesis but experimental lacking some useful details

The preparation of tetramethylguanidium azide was successfully carried out following the literature preparation (JOC 31, 1426 (1966)).  Hydrazoic acid was prepared as a Et2O solution by adding conc HCl over 30 minutes to a ice cold solution of NaN3 in...

LC-MS method for core metabolites; readily implemented.

A method for LCMS analysis and quantification of core metabolites (e.g. NADH/NAD, glycolysis, citrate cycle, etc.) was presented by the authors. I established their method on our own device, which worked well and only required the device-specific typical...

Wide versatility and good reproducibility

This work by Lafrance and co-work represents a very mild means to induce the decarboxylation of malonic acid derivatives with 1,1-carbonyldiimidazole (CDI). The reactive intermediate carbonyl imidazole moiety can be trapped with various nucleophiles in an...

Synthesis of poly(m-aniline) Table 1, Run 1

Under nitrogen, 1,3-dichlorobenzene (1 mmol) and 1,3-diaminobenzene were dissolved in toluene (15 mL). Sodium-tert-butoxide (NaO-t-Bu) (3 mmol), Ni(cod)2 (0.1 mmol), and DPPF (0.3mmol) were added to the solution at room temperature. The reaction mixture was...

Replicable (w/ Minor Modifications)

This paper was about first total synthesis of an indole alkaloid, Spirobacillene A and the key step of this approach was a Lewis acid catalyzed spirocyclization of an anisole derivative onto a tethered ynone.

I tried to replicate some of these reactions...

Good synthesis of enantiomerically pure (R)-sumanirole

PNU-95666E (sumanirole) was reported to be a highly selective D2 receptor full agonist. It was originally developed for the treatment of Parkinson’s disease. An eight steps synthesis was developed for the scale up of enantiomerically pure (R)-sumanirole with...

Aspirin

Synthesis of N-alkylated Benzodiazepines

I used this published synthetic method for making similar N-alkylated benzodiazepine molecules. The reaction was very reliable and good yielding in case of exact molecule but in my molecule, which was basically 1,4-benzodiazepine-2-one derivative, this...

Few Experimental Modifications Implemented to Improve Yield

Synthesized (3) and a compound similar to (4) but with protection on -OH groups. 

For (3): Dissolving CBr4 in dichloromethane instead of pyridine gave a better yield as it involved using only one solvent throughout the reaction. 

For (4): The formation...

Butane 2,3-Bisacetal Protection of Vicinal Diequatorial Diols

Authours: Jean-Luc Montchamp, Feng Tian, Matthew E. Hart, and J. W. Frost* 

Journal: J. Org. Chem. 1996, 61, 3897-3899 

After searching for an alternate protecting group for the protection of cis-dihydrocatechols, it was found that the butane-bisacetals...

Strain rate/ impact loading dependency of polyurea

This communication was outstanding in providing a comprehensive study of polyurea properties for: 

1) Development of constitutive model for polyurea at high strain rate loading conditions

2) Study of polyurea behavior from a quasi-static to ultra high...