Screening Substrates - QChASM/Aaron GitHub Wiki

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Overview

Another common use of AARON is to make predictions for a given ligand/catalyst for different substrates. This can be done for any substrate that can be formed by performing substitutions on the substrate present in the TS template library. The substitutions are specified within the a '&Substrates' section of the AARON input file.

Example 1: Screening Multiple Substrates

We will again use the bipyridine-N,N'-dioxide catalyzed allylation of aromatic aldehydes as an example. This time, however, we'll consider benzaldehydes with substitutions at atom 14:

AARON Input File

Note that you need always to specify at least one ligand. This ligand can be just the ligand present in the TS library ('None') or some new ligand or substituted ligand.

The input file below will request all TS structures be computed for the allylation of substituted benzaldehyde for substrates constructed by replacing atom 14 with CN and F using the ligand present in the TS library (bipyridine-N,N'-dioxide):

reaction_type=Allylation
template=NN-dioxide_example
charge=1
method=b97d
denfit=true
basis=6-31G
&Ligands
Cat1: None
&
&Substrates
Sub1: 14=CN
Sub2: 14=F
&

Example 2: Screening multiple ligands over multiple substrates

AARON can also screen multiple catalysts/ligands over multiple substrates.

We will consider the same two substrates as in Example 1, but now we will make predictions for bi-isoquinoline-N,N'-dioxide and a fluorinated analogue.

AARON Input File

reaction_type=Allylation
template=NN-dioxide_example
charge=1
method=b97d
denfit=true
basis=6-31G
&Ligands
Cat3: ligand=bi-isoquinoline-NN-dioxide
Cat4: ligand=bi-isoquinoline-NN-dioxide 14=F 17=F
&
&Substrates
Sub1: 14=CN
Sub2: 14=F
&

Note that AARON will actually make predictions for six different systems. First, it will compute all TS structures for the new catalysts with the original substrate found in the TS library:

 Cat3/Cat3
 Cat4/Cat4

It will then use these structures as templates for the two new catalysts applied to the two new substrates formed by performing the requested substitutions:

 Cat3/Cat3-Sub1
 Cat3/Cat3-Sub2
 Cat4/Cat4-Sub1
 Cat4/Cat4-Sub2

Notes on Rotamers

In general, AARON will also automatically detect and rotate any rotatable substituent on the catalyst/ligand (regardless of whether you added it or not!).

For the substrate, however, only newly added substituents will be rotated. This has important implications when you replace equivalent hydrogens.

For instance, suppose you have a TS library with a Me group on the substrate. If you want to make predictions for a benzyl group at this position, your first instinct might be to request that AARON replace one of the hydrogens of the Me group with Ph. However, this will result in AARON only considering rotamers of the added Ph group. In reality, you will want to consider the rotamers of the new benzyl group. As such, in such cases you should request that AARON replace the Me group with Bn.

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