Hydrogen bond strength as a function of ring size.

January 3rd, 2013

One frequently has to confront the question: will a hydrogen bond form between a suitable donor (lone pair or π) and an acceptor? One of the factors to be taken into consideration for hydrogen bonds which are part of a cycle is the ring size. Here I explore one way of quantifying the effect for the series below, n=1-5 (4-8 membered rings).

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Sharpless epoxidation, enantioselectivity and conformational analysis.

January 3rd, 2013

I return to this reaction one more time. Trying to explain why it is enantioselective for the epoxide product poses peculiar difficulties. Most of the substituents can adopt one of several conformations, and some exploration of this conformational space is needed.

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How to tame an oxidant: the mysteries of “tpap” (tetra-n-propylammonium perruthenate).

December 24th, 2012

tpap[cite]10.1055%2Fs-1994-25538[/cite], as it is affectionately known, is a ruthenium-based oxidant of primary alcohols to aldehydes discovered by Griffith and Ley. Whereas ruthenium tetroxide (RuO4) is a voracious oxidant[cite]10.1139/v76-304[/cite], its radical anion countered by a tetra-propylammonium cation is considered a more moderate animal[cite]10.1021/jo00038a009[/cite]. In this post, I want to try to use quantum mechanically derived energies as a pathfinder for exploring what might be going on (or a reality-check if you like). 

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Vitamin B12 and the genesis of a new theory of chemistry.

December 20th, 2012

I have written earlier about dihydrocostunolide, and how in 1963 Corey missed spotting the electronic origins of a key step in its synthesis.[cite]10.1021/ja00952a037[/cite]. A nice juxtaposition to this failed opportunity relates to Woodward’s project at around the same time to synthesize vitamin B12. The step in the synthesis that caused him to ponder is shown below.

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Non covalent interactions in the Sharpless transition state for asymmetric epoxidation.

December 19th, 2012

The Sharpless epoxidation of an allylic alcohol had a big impact on synthetic chemistry when it was introduced in the 1980s, and led the way for the discovery (design?) of many new asymmetric catalytic systems. Each achieves its chiral magic by control of the geometry at the transition state for the reaction, and the stabilizations (or destabilizations) that occur at that geometry. These in turn can originate from factors such as stereoelectronic control or simply by the overall sum of many small attractions and repulsions we call dispersion interactions. Here I take an initial look at these for the binuclear transition state shown schematically below.

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Why the Sharpless epoxidation is enantioselective!

December 17th, 2012

Part one on this topic showed how a quantum mechanical model employing just one titanium centre was not successful in predicting the stereochemical outcome of the Sharpless asymmetric epoxidation. Here in part 2, I investigate whether a binuclear model might have more success. The new model is constructed using two units of Ti(OiPr)4, which are likely to assemble into a dimer such as that shown below (in this crystal structure, some of the iPr groups are perfluorinated).

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Why is the Sharpless epoxidation enantioselective? Part 1: a simple model.

December 9th, 2012

Sharpless epoxidation converts a prochiral allylic alcohol into the corresponding chiral epoxide with > 90% enantiomeric excess[cite]10.1021/jo00369a032[/cite],[cite]10.1021/jo00360a058[/cite]. Here is the first step in trying to explain how this magic is achieved.

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The mechanism of the Birch reduction. Sequel to benzene reduction.

December 5th, 2012

I noted briefly in discussing why Birch reduction of benzene gives 1,4-cyclohexadiene (diagram below) that the geometry of the end-stage pentadienyl anion was distorted in the presence of the sodium cation to favour this product. This distortion actually has some pedagogic value, and so I elaborate this here.

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The mechanism of the Birch reduction. Part 3: reduction of benzene

December 4th, 2012

Birch reduction of benzene itself results in 1,4-cyclohexadiene rather than the more stable (conjugated) 1,3-cyclohexadiene. Why is this?

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The mechanism of the Birch reduction. Part 2: a transition state model.

December 3rd, 2012

I promised that the follow-up to on the topic of Birch reduction would focus on the proton transfer reaction between the radical anion of anisole and a proton source, as part of analysing whether the mechanistic pathway proceeds O or M.

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